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IDPMIDYEARSequenceNameLengthN-ter MODC-ter MODLinear/CyclicChiralityChem-MODOriginNatureIncubation TimeConcentrationHalf LifeUnits Half LifeProteaseAssayTest SampleVivo/VitroReferencePatent No.Activity
1001
208447652010
RRWQWR
Lfc16FreeFreeLinearLNoneBovine lactoferricinAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=60μM for E.coli
1002
208447652010
RRWQWR
Lfc16FreeFreeLinearLNoneBovine lactoferricinAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=30μM for S. aureus
1003
208447652010
RRWQWR
Lfc16FreeFreeLinearLNoneBovine lactoferricinAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=7.5 μM for B. subtilis
1004
208447652010
RRWWRF
Com16FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=60μM for E.coli
1005
208447652010
RRWWRF
Com16FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=7.5μM for S. aureus
1006
208447652010
RRWWRF
Com16FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=1.9 μM for B. subtilis
1007
208447652010
RRWQWR
Lfc26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=15μM for E.coli
1008
208447652010
RRWQWR
Lfc26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=15μM for S. aureus
1009
208447652010
RRWQWR
Lfc26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=1.9μM for B. subtilis
1010
208447652010
RRWWRF
Com26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=30μM for E.coli
1011
208447652010
RRWWRF
Com26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=30μM for S. aureus
1012
208447652010
RRWWRF
Com26FreeAmidationLinearLNoneSyntheticAntimicrobial9 hours5 µM<30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=0.9 μM for B. subtilis
1013
208447652010
RRWQWR
Lfc36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=120μM for E.coli
1014
208447652010
RRWQWR
Lfc36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99>120μM for S. aureus
1015
208447652010
RRWQWR
Lfc36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=60 μM for B. subtilis
1016
208447652010
RRWWRF
Com36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=120μM for E.coli
1017
208447652010
RRWWRF
Com36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=30μM for S. aureus
1018
208447652010
RRWWRF
Com36AcetylationFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM~60Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=7.5μM for B. subtilis
1037
208447652010
RRWQWRMKKLG
Lfc711FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM>30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=15μM for E.coli
1038
208447652010
RRWQWRMKKLG
Lfc711FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM>30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=7.5μM for S. aureus
1039
208447652010
RRWQWRMKKLG
Lfc711FreeFreeLinearLNoneSyntheticAntimicrobial9 hours5 µM>30Human serum proteasesRP-HPLCHuman serumin vitroNoneNoneLD99.99=0.9μM for B. subtilis
1056
122701692002
ALCDNPRIDRWYCQFVEG
Peptide 1a18AcetylationAmidationLinearLNoneSyntheticAnticoagulantNot reported5mg/kg7.6Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=1.1nM for fVIIa binding assay
1057
122701692002
ALCDNPRIDRWYCQFVEG
Peptide 1b18Acetylation [(C6H6)2-CO-]AmidationLinearLNoneSyntheticAnticoagulantNot reported5mg/kg15Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=4nM for fVIIa binding assay
1058
122701692002
ALCDNPRIDRWYCQFVEG
Peptide 1c18Acetylation [(CH3)2-CH-CH2-(C6H6)-CH(CH3)-CO]AmidationLinearLNoneSyntheticAnticoagulantNot reported4.9mg/kg24Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=14.6nM for fVIIa binding assay
1059
122701692002
ALCDNPRIDRWYCQFVEG
Peptide 1c18Acetylation [(CH3)2-CH-CH2-(C6H6)-CH(CH3)-CO]AmidationLinearLNoneSyntheticAnticoagulantNot reported2mg/kg17Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=14.6nM for fVIIa binding assay
1060
122701692002
ALCDNPRIDRWYCQFVEG
Peptide 1m18Acetylation (Napthalene acyl sulfonamide)AmidationLinearLNoneSyntheticAnticoagulantNot reported2mg/kg30Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=1.0nM for fVIIa binding assay
1061
126997442003
ALCDNPRIDRWYCQFVEG
Peptide 1a18AcetylationAmidationLinearLNoneSyntheticAnticoagulantNot reported1.11mg/kg4.18Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=9.7nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin
1062
126997442003
ALCDNPRIDRWYCQFVEG
Peptide 1b18Acetylation(Naphthalene acylsulfonamide)AmidationLinearLNoneSyntheticAnticoagulantNot reported2mg/kg30Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=24nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin
1064
126997442003
ALCDNPRIDRWYCQFVEG
Peptide 5b18Acetylation (Naphthalene)AmidationLinearLNoneSyntheticAnticoagulantNot reported2mg/kg34.8Rabbit blood proteasesELISAIntravenouly administered into rabbit bloodin vivoNoneNoneIC50=9.2nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin
1066
153221252004
DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVV
Aβ(1 €“ 40)40FreeFreeLinearLNoneDerivative of human A precursor protein APP770Neurodegenerative120 minutes2x107 cpm of 125I-Aβ42 peptide2.4Mouse plasma proteasesRadioactivity measured by scintillation counterIntravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samplesin vivoNoneNoneNeurodegeneration caused by oligomerization
1067
153221252004
DAEFRHDSGYEVHHQKLVFFAEDVGSNKGAIIGLMVGGVVIA
Aβ(1 €“ 42)42FreeFreeLinearLNoneDerivative of human Aprecursor protein APP771Neurodegenerative121 minutes2x107 cpm of 125I-Aβ40 peptide2.8Mouse plasma proteasesRadioactivity measured by scintillation counterIntravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samplesin vivoNoneNoneNeurodegeneration caused by oligomerization
1074
150125922004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeFreeLinearLNoneGlucagonAntihyperglycaemic, insulinotropicNot reported25 nM/kg body weight< 2Adult obese diabetic (ob /ob ) mice blood proteaseLC/MS equipped with a microbore C-18 HPLCIntraperitoneally administered to adult obese diabetic (ob /ob ) micein vivoNoneNoneIC50 = 0 ·37 nM of binding to a receptor
1078
21476961990
PINPRLDG
Control peptide8FreeFreeLinearLNoneSynthetic peptide (scrambled amino acids of human protein S)AnticoagulantNot reportedNot mentioned15Rabbit blood proteasesSpectrofluorometryIntravenously injected in male New Zealand white rabbits and blood samples withdrawn and plasma sample preparedin vivoNoneNoneNo activity found
1079
21476961990
DGEQLADLIV
Control peptide10FreeFreeLinearLNoneSynthetic peptide (amino acids 400-407 of human protein S)AnticoagulantNot reportedNot mentioned15Rabbit blood proteasesSpectrofluorometryIntravenously injected in Male New Zealand white rabbits and blood samples withdrawn and plasma sample preparedin vivoNoneNoneNo activity found
1080
115536912001
KKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQNIATVIVITLVML
APP-C5959FreeFreeLinearLNoneAmyloid precursor protein derivativeRegulator of synapse formation2 hoursNot mentioned~5Fetal calf serum proteasesPulse chase experimentBHK cell linein vitroNoneNoneNot reported
1081
115536912001
KKKQYTSIHHGVVEVDAAVTPEERHLSKMQQNGYENPTYKFFEQMQNIATVIVITLVML
APP-C5959FreeFreeLinearLNoneAmyloid precursor protein derivativeRegulator of synapse formation2 hoursNot mentioned~5Fetal calf serum proteasesPulse chase experimentPrimary cultures of neurons from PS1 knockout mice's 14 day embryosin vitroNoneNoneNot reported
1086
120397082002
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Glucagon-like peptide-1 (GLP-1)30FreeAmidationLinearLNoneDerived from proteolytic cleavage of proglucagonInsulinotropicNot reportedNot mentioned1.5 €“5Plasma proteasesRadioimmunoassayRat plasmain vivo24199154NoneGLP-1 normalizes blood glucose levels
1087
128594282003
SPKMMHKSGCFGRRLDRIGSLSGLGCNVLRKY
BNP-3232FreeFreeLinearLNoneCanine B-type natriuretic peptideDiuretic, natriuretic, hypotensive and smooth muscle relaxant activitiesNot reportedNot mentioned1.57 ± 0.14Dog plasma proteasesRadioimmunoassayInjected intravenously into dogsin vivoNoneNone44.7 ±0.3% RBC during BNP-32 infusion
1094
125788302003
LPFFD
iAβ5p-C15FreeAmidationLinearLNoneSyntheticβ-sheet breaker peptidesNot reported20 nmol5Human plasma proteasesRP-HPLCHuman plasmain vitroNoneNone>80% inhibition of amyloid fibrillogenesis
1097
125788302003
LPFFD
iAβ5p5FreeFreeLinearLNoneSyntheticβ-sheet breaker peptidesNot reported20 nmol15Human plasma proteasesRP-HPLCHuman plasmain vitroNoneNone100% inhibition of amyloid fibrillogenesis
1103
125788302003
LPFFD
iAβ5p-C15FreeAmidationLinearLNoneSyntheticβ-sheet breaker peptidesNot reported20 nmol<1Proteases in rat brain homogenateRP-HPLCRat brain homogenatein vitroNoneNone>80% inhibition of amyloid fibrillogenesis
1104
125788302003
Sar-LPFFD
iAβ5p-C25SarAmidationLinearLNoneSyntheticβ-sheet breaker peptidesNot reported20 nmol41Proteases in rat brain homogenateRP-HPLCRat brain homogenatein vitroNoneNone>80% inhibition of amyloid fibrillogenesis
1105
125788302003
(Nme)-Sar-LPFFD
iAβ5p-C35(NMe)SarAmidationLinearLNoneSyntheticβ-sheet breaker peptidesNot reported20 nmol25Proteases in rat brain homogenateRP-HPLCRat brain homogenatein vitroNoneNone>80% inhibition of amyloid fibrillogenesis
1113
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=3 µg/ml for M. Luteus ATCC 9341
1114
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=4 µg/ml for M. Luteus ATCC 9341
1115
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=7 µg/ml for M. Luteus ATCC 9341
1118
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=3 µg/ml for M. Luteus ATCC 9343
1120
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=6 µg/ml for M. Luteus ATCC 9345
1121
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=6.25 µg/ml for S. Aureus ATCC 6538
1122
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=9 µg/ml for S. Aureus ATCC 6538
1123
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=19 µg/ml for S. Aureus ATCC 6539
1126
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=10 µg/ml for S. Aureus ATCC 6542
1128
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=11 µg/ml for S. Aureus ATCC 6544
1129
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=1.56 µg/ml for S. Epidemidis ATCC 12228
1130
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=1.56 µg/ml for S. Epidemidis ATCC 12229
1131
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=3.12 µg/ml for S. Epidemidis ATCC 12228
1134
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=1.56 µg/ml for S. Epidemidis ATCC 12229
1136
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneNot reported
1137
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 µg/ml for MRSA SR 1550
1138
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=50 µg/ml for MRSA SR 1551
1139
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=100 µg/ml for MRSA SR 1552
1142
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=42 µg/ml for MRSA SR 1555
1144
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=16 µg/ml for MRSA SR 1557
1145
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for M. smegmatis ATCC 607
1146
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 µg/ml for M. smegmatis ATCC 607
1147
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=>100 µg/ml for M. smegmatis ATCC 607
1150
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for M. smegmatis ATCC 612
1152
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneNot reported
1153
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=10 µg/ml for E. coli ATCC 2592
1154
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for E. coli ATCC 2592
1155
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=23 µg/ml for E. coli ATCC 2592
1158
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=21 µg/ml for E. coli ATCC 2592
1160
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=11 µg/ml for E. coli ATCC 2592
1161
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=4 µg/ml for P. aeruginosa ATCC 9027
1162
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for P. aeruginosa ATCC 9027
1163
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=20 µg/ml for P. aeruginosa ATCC 9027
1166
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=10 µg/ml for P. aeruginosa ATCC 9027
1168
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=5 µg/ml for P. aeruginosa ATCC 9027
1169
104617471998
KKVVFKVKFK
KSL10FreeFreeLinearLNoneSyntheticAntimicrobialNot reported100 µg/mL6Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for C. albicans ATCC 36232
1170
104617471998
KΨ[CH2NH]KVVFKVKFK
KSL110FreeFreeLinearLReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL14Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=9 µg/ml for C. albicans ATCC 36232
1171
104617471998
KΨ[CH2NH]KVVFKVKFk
KSL210FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=17 µg/ml for C. albicans ATCC 36232
1174
104617471998
KΨ[CH2OCONH]KVVFKVKFk
KSL510FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL23Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=10 µg/ml for C. albicans ATCC 36232
1176
104617471998
kKVVFKVKFk
KSL710FreeFreeLinearMixNoneSyntheticAntimicrobialNot reported100 µg/mL22Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for C. albicans ATCC 36232
1181
107730092000
TaLIDNNATEEILY
TX14(A)14FreeFreeLinearMixNoneSynthetic derivative of prosaposinNeurotrophic factor9 minutesNot mentioned4.2 ±0.3Rat serum proteasesRadioactivity measured with a gamma counterInjected in jugular vein of male Sprague-Dawley ratsin vivoNoneNoneED50=1.00 ±0.11ng/ml
1182
107730092000
TaIIDNNKTEKEISY
TX15-215FreeFreeLinearMixNoneSynthetic derivative of prosaposinNeurotrophic factor9 minutesNot mentioned2.5 ±0.3Rat serum proteasesRadioactivity measured by a gamma counterInjected in jugular vein of male Sprague-Dawley ratsin vivoNoneNoneED50=1.00 ±0.09ng/ml
1185
110546372000
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Human brain natriuretic peptide (hBNP)32FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned12.7Sheep blood proteasesHPLCInfused in pulmonary artery of sheepin vivo2136732NoneKd=8pM for receptor binding
1186
110546372000
MMRDSGCFGRRLDRIGSLSGLGCNVLRRY
Ovine Brain natriuretic peptide (oBNP)29FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned2.6Sheep blood proteasesHPLCInfused in pulmonary artery of sheepin vivoNoneNoneKd=16pM for receptor binding
1187
110546372000
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial natriuretic peptide (ANP)28FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned3Sheep blood proteasesHPLCInfused in pulmonary artery of sheepin vivo1826098NoneKd=10pM for receptor binding
1188
110546372000
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Human brain natriuretic peptide (hBNP)32FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned3.1Human blood proteasesHPLCInjected in humansin vivo2136732NoneKd=8pM for receptor binding
1189
110546372000
MMRDSGCFGRRLDRIGSLSGLGCNVLRRY
Ovine Brain natriuretic peptide (oBNP)29FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned3.1Human blood proteasesHPLCInjected in humansin vivoNoneNoneKd=16pM for receptor binding
1190
110546372000
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial natriuretic peptide (ANP)28FreeFreeLinearLNoneCardiac originRegulation of extracellular fluid and blood pressure homeostasisNot mentionedNot mentioned22Human blood proteasesHPLCInjected in humansin vivo1826098NoneKd=10pM for receptor binding
1191
106707531999
SPTLAYAVP
Human thyrotropin-releasing hormone (TRH)-associated peptide 3 (hTAP-3)9FreeFreeLinearLNoneProduct of proteolysis of preproTRHSerum hTAP-3 concentration was increased in patients with hyperthyroidism15 minNot mentioned3.5Human serum proteasesRadioimmunoassayHuman serumin vivoNoneNoneNot reported
1192
149807872004
LW
Leucyl-tryptophane2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned7.4Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=15 µM
1193
149807872004
SY
Seryl-tyrosine2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned5.2Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=41 µM
1194
149807872004
VY
Valyl-tyrosine2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned15Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=11 µM
1195
149807872004
LY
Leucyl-tyrosine2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned4.3Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=44 µM
1196
149807872004
AY
Alanyl-tyrosine2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned9.4Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=40 µM
1197
149807872004
YY
Tyrosyl-tyrosine2FreeFreeLinearLNoneSyntheticAngiotensin Coverting Enzyme inhibitorNot mentionedNot mentioned16Rat plasma proteasesSpectrophotometryRat plasmain vitroNoneNoneIC50=9 µM
1200
203826952010
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
hGLP-1(7-36)NH230FreeAmidationLinearLNoneGlucagon like peptide-1Regulate blood glucoseNot mentionedNot mentioned50Rat plasma proteaseRP-HPLCRat plasmain vitro14759771NoneEC50=0.08nM for stimulating cAMP production
1203
204189552010
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNoneGlucagonRegulate blood glucoseNot mentionedNot mentioned<10Not reportedNot mentionedNot reportedin vivoNoneNoneElevated blood glucose levels for <2 hours
1210
211145992010
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
hGLP-1(7-36)NH230FreeAmidationLinearLNoneGlucagon like peptide-1Regulate blood glucoseNot mentionedNot mentioned0.9 ±0.1Rat plasma proteasesHPLCRat plasmain vitro14759771NoneEC50=0.08 ±0.03nM for cAMP stimulation
1218
205876452010
VRRADRAAVPGGGGRG
HM-316FreeFreeLinearLNoneDerivative of endostatinAnti-angiogeneticNot mentionedNot mentioned10 to 27SD rat plasma proteasesRP-HPLCSD rat plasmain vitrohttp://pubs.rsc.org/En/content/articlepdf/2014/tb/None39.68% inhibitory effect on mouse tumors
1221
205934702010
GGFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS
Peptide 141FreeAmidationLinearLNoneSynthetic dipeptide extended GLP-analogsRegulate blood glucose168 hoursNot mentioned0.9NoneHPLCPBSin vitroNoneNoneNot reported
1223
205934702010
GFFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS
Peptide 341FreeAmidationLinearLNoneSynthetic dipeptide extended GLP-analogsRegulate blood glucose168 hoursNot mentioned0.7NoneHPLCPBSin vitroNoneNoneNot reported
1224
205934702010
GfFAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS
Peptide 441FreeAmidationLinearMixNoneSynthetic dipeptide extended GLP-analogsRegulate blood glucose168 hoursNot mentioned0.9NoneHPLCPBSin vitroNoneNoneNot reported
1228
205934702010
G-PhG-FAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS
Peptide 841FreeAmidationLinearLPhG=phenylglycineSynthetic dipeptide extended GLP-analogsRegulate blood glucose168 hoursNot mentioned0.5NoneHPLCPBSin vitroNoneNoneNot reported
1229
205934702010
G-Aib-FAEGTFTSDVSSYLEGQAAKEFIAWLVKGRPSSGAPPPS
Peptide 941FreeAmidationLinearLAib=α-aminoisobutyric acidSynthetic dipeptide extended GLP-analogsRegulate blood glucose168 hoursNot mentioned0.8NoneHPLCPBSin vitroNoneNoneNot reported
1246
172929772007
HGEGTFTSDLSKQLEEEAVRLFIEWLKNGGPSSGAPPPS
AC317439FreeAmidationLinearLNoneAnalog of exendin-4Regulates blood glucoseNot mentionedNot mentioned42 ±3.4Rat plasma proteasesELISASubcutaneously administion of 10 µg/kg dose to Sprague Dawley ratsin vivoNoneNoneED50=1.2 µg/kg for glucose lowering in db/db mice
1247
172929772007
HGEGTFTSDLSKQLEEEAVRLFIEWLKNGGPSSGAPPPS
AC317439FreeAmidationLinearLNoneAnalog of exendin-4Regulates blood glucoseNot mentionedNot mentioned43 ±4.0Rat plasma proteasesELISASubcutaneously administion of 100 µg/kg dose to Sprague Dawley ratsin vivoNoneNoneED50=1.3 µg/kg for glucose lowering in C57BL/6 mice
1248
222860342012
FVPIFTYGELQRMQEKERNKGQ
Motilin22FreeFreeLinearLNoneMotilin is a gastro-intestinal peptide hormoneEndocrine regulator of gastro-intestinal motilityNot mentioned10 nmol/kg3.3 ±1.0Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=8.9x10-11nM for GPR38 agonist activity
1249
222860342012
FVPIFTYGELQRSPEHQRVQQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(6 €“28)35FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg11.7 ±3.4Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.5x10-9nM for GPR38 agonist activity
1250
222860342012
FVPIFTYGELQREHQRVQQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(8 €“28)33FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg11.1 ±0.7Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.4x10-10nM for GPR38 agonist activity
1251
222860342012
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(10 €“28)31FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg8.9 ±0.5Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.6x10-10nM for GPR38 agonist activity
1252
222860342012
FVPIFTYGELQRVQQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(12 €“28)29FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg8.9 ±0.5Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=8.6x10-11nM for GPR38 agonist activity
1253
222860342012
FVPIFTYGELQRQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(14 €“28)27FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg8.0 ±0.7Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=6.1x10-10nM for GPR38 agonist activity
1254
222860342012
FVPIFTYGELQRKESKKPPAKLQPR
Motilin(1 €“12)ghrelin(16 €“28)25FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg9.4 ±0.6Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.2x10-9nM for GPR38 agonist activity
1255
222860342012
FVPIFTYGELQRSKKPPAKLQPR
Motilin(1 €“12)ghrelin(18 €“28)23FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg5.3 ±1.3Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.0x10-10nM for GPR38 agonist activity
1256
222860342012
FVPIFTYGELQRKKPPAKLQPR
Motilin(1 €“12)ghrelin(19 €“28)22FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg6.0 ±0.3Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.1x10-10nM for GPR38 agonist activity
1257
222860342012
FVPIFTYGELQRVQQRKESKKPPAKLQ
Motilin(1 €“12)ghrelin(12 €“26)27FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg10.4 ±0.1Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=8.5x10-9nM for GPR38 agonist activity
1258
222860342012
FVPIFTYGELQRVQQRKESKKPPAK
Motilin(1 €“12)ghrelin(12 €“24)25FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg5.8 ±0.7Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=4.8x10-11nM for GPR38 agonist activity
1259
222860342012
FVPIFTYGELQRVQQRKESKKPP
Motilin(1 €“12)ghrelin(12 €“22)23FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg6.3 ±0.5Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=2.4x10-11nM for GPR38 agonist activity
1260
222860342012
FVPIFTYGELQRVQQRKESKK
Motilin(1 €“12)ghrelin(12 €“20)21FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg7.0 ±2.6Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=7.3x10-11nM for GPR38 agonist activity
1261
222860342012
FVPIFTYGELQRVQQRKES
Motilin(1 €“12)ghrelin(12 €“18)19FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg3.1 ±0.7Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=8.8x10-10nM for GPR38 agonist activity
1262
222860342012
FVPIFTYGELQRVQQRK
Motilin(1 €“12)ghrelin(12 €“16)17FreeFreeLinearLNoneChimeric peptide of motilin and ghrelinRegulator of gastro-intestinal motilityNot mentioned10 nmol/kg2.4 ±0.7Rat plasma proteasesRadioimmunoassayIntravenouly injected in Sprague-Dawley ratsin vivoNoneNoneEC50=1.2x10-10nM for GPR38 agonist activity
1263
171077182006
HADGSFSDEMNTILDNLAARDFINWLIQTKITD
Glucagon-like peptide-2 (GLP-2)33FreeFreeLinearLNonePosttranslational processing of proglucagonStimulate intestinal growthNot mentionedNot mentioned6.8 ±0.8Pig plasma proteasesELISAInfused into blood of pigsin vivoNoneNoneNot reported
1264
171077182006
HADGSFSDEMNTILDNLAARDFINWLIQTKITD
Glucagon-like peptide-2 (GLP-2)33FreeFreeLinearLNonePosttranslational processing of proglucagonStimulate intestinal growthNot mentionedNot mentioned9.9 ±0.8Pig plasma proteases with valine-pyrrolidide (DPP-IV inhibitor)ELISAInfused into blood of pigsin vivoNoneNoneNot reported
1265
144997072003
YADAIFTNSYRKVLGQLSARKLLQDIMSR
GRF1-2929FreeAmidationLinearLNoneGrowth hormone-releasing hormone (GRF) analogueStimulates release of growth hormoneNot mentionedNot mentioned10 to 20Human plasma proteasesNot mentionedHuman plasmain vivoNoneNoneEC50=0.18nM
1644
225922002012
GSSFLSPEHQKAQQRKESKKPPAKLQPR
Ghrelin28FreeFreeLinearLFatty acid ie n-octanoic acid present at serine at position 3, (125)I labellingGhrelinGH-releasing and appetite stimulating peptideNot reportedNot mentioned15-18Rat blood proteasesRadioactivity measured by scintillation counterAdministered into blood of ratsin vivo15788704NoneNot reported
1647
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml1.17 ±0.08Proteases in rat intestinal fluidRP-HPLCRat intestinal fluidin vitroNoneNoneIntraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2%
1648
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml1.34 ±0.07Proteases in rat intestinal homogenateRP-HPLCRat intestinal homogenatein vitroNoneNoneIntraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2%
1649
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys26,34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th and 26th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml4.34 ±0.21Proteases in rat intestinal fluidRP-HPLCRat intestinal fluidin vitroNoneNoneOral hypoglycemic efficacy in db/db mice was 25.3 ±6.6%
1650
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys26,34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th and 26th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml2.77 ±0.05Proteases in rat intestinal homogenateRP-HPLCRat intestinal homogenatein vitroNoneNoneOral hypoglycemic efficacy in db/db mice was 25.3 ±6.6%
1653
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml1.17 ±0.08Proteases in rat intestinal fluidRP-HPLCRat intestinal fluidin vitroNoneNoneEC50=3.82 ±0.32nM insulinotropic activity
1654
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml1.34 ±0.07Proteases in rat intestinal homogenateRP-HPLCRat intestinal homogenatein vitroNoneNoneEC50=3.82 ±0.32nM insulinotropic activity
1655
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys26,34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th and 26th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml4.34 ±0.21Proteases in rat intestinal fluidRP-HPLCRat intestinal fluidin vitroNoneNoneEC50=3.85 ±0.21nM insulinotropic activity
1656
179043402008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys26,34-biotin-GLP-130FreeAmidationLinearLBiotinylation at Lys at 34th and 26th positionBiotinylated derivative of GLP-1Regulates blood glucose levelsNot reported200 µg/ml2.77 ±0.05Proteases in rat intestinal homogenateRP-HPLCRat intestinal homogenatein vitroNoneNoneEC50=3.85 ±0.21nM insulinotropic activity
1657
205851282010
RRWRIVVIRVRR
Sub312FreeAmidationLinearLNoneDerived from bovine peptide bactenecinAntimicrobialNot reported150 µg/ml~60Proteases in mouse serumRP-HPLC25% aqueous mouse serumin vitroNoneNoneMIC=1 µg/ml for S. Aureus
1659
205851282010
aRRWRIVVIRVRRh
Sub3-D14FreeAmidationLinearMixNoneDerivative of Sub4AntimicrobialNot reported150 µg/ml~60Proteases in mouse serumRP-HPLC25% aqueous mouse serumin vitroNoneNoneMIC=1 µg/ml for S. Aureus
1661
205851282010
RRWRIVVIRVRR
Sub312FreeAmidationLinearLNoneDerived from bovine peptide bactenecinAntimicrobialNot reported150 µg/ml~60Proteases in mouse serumRP-HPLC25% aqueous mouse serumin vitroNoneNoneMIC=2 µg/ml for P. Aeruginosa
1663
205851282010
aRRWRIVVIRVRRh
Sub3-D14FreeAmidationLinearMixNoneDerivative of Sub4AntimicrobialNot reported150 µg/ml~60Proteases in mouse serumRP-HPLC25% aqueous mouse serumin vitroNoneNoneMIC=2 µg/ml for P. Aeruginosa
1676
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~60 ±1Angiotensin-converting enzyme and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of normotensive Sprague-Dawley ratin vivoNoneNoneNot mentioned
1682
98069491998
NDWF-Dpr-L
MEN 114206GlycosylationFreeCyclicLDpr-2,3-Diaminopropionic acidMEN 10627Tachykinin NK2 receptor antagonistNot reportedNot mentioned44 ±3Not mentionedHPLCRat blood plasmain vivoNoneNoneNot mentioned
1683
98226651998
MLPGLALLLLAAWTARALEVPYPYDVPDYASNKGAIIGLMVGGVVIATVIVITLVVMLKKKQYEQKLISEEDL
H26-57C74FreeFreeLinearLNoneAmyloid precursor proteinNot mentioned40 minutesNot mentioned8γ-secretasePulse chase experimentHuman embryonic kidney cellsin vitroNoneNoneNot mentioned
1684
98226651998
MLPGLALLLLAAWTARALEVPYPYDVPDYASNKGAIIGLMVGGVVIATVIVITLVVMLKKKQYEQKLISEEDL
H26-57C74FreeFreeLinearLNoneAmyloid precursor proteinNot mentioned40 minutesNot mentioned1γ-secretase (protease) Lactacystin(protease inhibitor)Pulse chase experimentHuman embryonic kidney cellsin vitroNoneNoneNot mentioned
1686
6596331978
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide31FreeFreeLinearLNoneProinsulinNot mentionedNot reported0.75pmol/ml33.5(mean)Not mentionedSingle-dose injection technique6 Normal human male blood plasma samplein vivoNoneNoneNot mentioned
1687
6596331978
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide31FreeFreeLinearLNoneProinsulinNot mentionedNot reported0.9pmol/ml42.5(mean)Not mentionedSingle-dose injection technique7 Diabetic human male blood plasma samplein vivoNoneNoneNot mentioned
1693
33433381987
GRGDS
Anti-cell adhesive pentapeptide5FreeFreeLinearLNoneCentral cell- binding domain of fibronectinAnti metastaticNot reported6 µmol8Not mentionedRadioactivity measured by scintillation counterBlood sample of C57BL/6 micein vivoNoneNonePercentage inhibition of melanotic colony formation=90
1694
60864051984
Glp-PPGGSKVILF
Hydra head activator11FreeFreeLinearLGlp-Pyroglutamic acidHydra but also found in rat intestine,human and bovine hypothalamusIn hydra-stimulatory effects on growth and differentition,in human-in digestion control process2 hour20-100 fmol/ml7Not mentionedRadioimmunoassayHuman plasmain vitroNoneNoneNot mentioned
1695
61175061981
AGCKNFFWKTFTSC
Somatostatin14FreeFreeCyclic (C3-C14)LNoneOvineLocal transmitters either paracrine or neurocrine5 days100ng1.0 ±0.2Not mentionedRadioimmunoassayBlood plasma sample from five mongrel dogsin vivo4682131NoneNot mentioned
1696
74393981980
ECG
Glutathione3FreeFreeLinearLGamma peptide linkage between the carboxyl group of the glutamate side-chain and the amine group of cysteineSyntheticNot mentionedNot reported25 ng/kg/min of Bradykinin and the rate doubled every 5 min until a final rate of 200 ng/kg/min was1.6Not mentionedKinetic assayHuman blood plasma samplein vivoNoneNoneNot mentioned
1699
82574271993
SDKP
AcSDKP4AcetylationFreeLinearLNoneHuman bone marrowNegative regulator of proliferation of haematopoietic stem cellsNot reported10nM conc.50NoneRadioactivity measured with liquid-scintillation counterHuman venous blood samplein vitroNoneNoneNot mentioned
1700
82574271993
SDKP
AcSDKP4AcetylationFreeLinearLNoneHuman bone marrowNegative regulator of proliferation of haematopoietic stem cellsNot reported10-4M conc10Rabbit lung angiotensin I converting enzymeRadioactivity measured with liquid-scintillation counterHuman venous blood samplein vitroNoneNoneNot mentioned
1701
82574271993
SDKP
AcSDKP4AcetylationFreeLinearLNoneHuman bone marrowNegative regulator of proliferation of haematopoietic stem cellsNot reported10-7M conc.25Rabbit lung angiotensin I converting enzymeRadioactivity measured with liquid-scintillation counterHuman venous blood samplein vitroNoneNoneNot mentioned
1705
106111391999
H(2me)wAWfK
Hexarelin6FreeAmidationLinearMix2me-2-methyl(tryptophan)Analog of GHRP-6Peptidyl growth hormone causing GH releasing effect.Not reported50 µg/kg57.0 ±9.1Blood proteasesLC-MS/MSIntravenous injection,Blood sample from male Sprague-Dawley ratsin vivoNoneNoneNot mentioned
1706
106476192000
GPRPP-Aba-GGaG
TP 85010FreeFreeLinearMix4-aminobutyric acid (Aba)Modified fibrin α chain N-terminal peptideBlood CoagulationNot reported11 to 25 iu of oxytocin4Blood proteasesRadiolabelling and HPLCIntravenous injection,Blood sample of rabbitin vivoNoneNonePlatelet aggregation inhibition, IC50=236μm for dog and IC50=167μm for rabbit.
1710
121193022002
ALCDNPRIDRWYCQFVEG
1a18AcetylationAmidationLinearLNoneSyntheticCoagulation factor VIIa peptide exosite inhibitorNot reported106 cpm/200μl/mouse7.6Blood proteasesESI-LC ˆ’MS/MSRabbit blood samplein vivoNoneNoneNot mentioned
1712
37992111986
YFQNCPrG
(I-deamino-8-D-arginine vasopressin)DDAVP91-β-mercaptopropionic acidFreeLinearMixNoneModified form of VasopressinAntidiuretic agentNot reported45mg55Plasma proteasesRadioimmunoassayHuman blood sampleN.A.NoneUS 5500413 A patentNot mentioned
1713
104540851999
CYIQNCPLG
Oxytocin9FreeAmidationCyclic (C1-C6)LNoneHypothalamusInvolved in aiding mechanical clearance mechanism and improving fertility60 minutes90mg6.78Blood proteaseRadioimmunoassayIntravenous injection of oxytocin in normal maresin vivoNoneNoneProstaglandin F metabolite(PGFM) release on administeration of 10 iu of oxytocin= 18.48 ±3.62 pg/ml
1714
104540851999
CYIQNCPLG
Oxytocin9FreeAmidationCyclic (C1-C6)LNoneHypothalamusInvolved in aiding mechanical clearance mechanism and improving fertility60 minutes180mg6.78Blood proteaseRadioimmunoassayIntravenous injection of oxytocin in normal maresin vivoNoneNoneProstaglandin F metabolite(PGFM) release on administeration of 25 iu of oxytocin= 20.09 ±3.29 pg/ml
1715
105440051999
YIGSR
YIGSR5FreeFreeLinearLNoneCore sequence located at the β-1 chain of lamininAntimetastatic effect.Not reportedNot mentioned<1Blood proteaseRadioactivity measured with a gamma counterIntravenous injection of labelled peptide in C57BL/6 micein vivoNoneNoneAt 1.5μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50%
1716
105440051999
YIGSR
PEG5000 -YIGSR5Pegylated by addition of PEG5000FreeLinearLNoneCore sequence located at the β-1 chain of lamininAntimetastatic effect.Not reportedNot mentioned2.2Blood proteaseRadioactivity measured with a gamma counterIntravenous injection of labelled peptide in C57BL/6 micein vivoNoneNoneAt 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx.
1717
105440052000
YIGSR
PEG12,000 -YIGSR5Pegylated by addition of PEG12,000FreeLinearLNoneCore sequence located at the β-1 chain of lamininAntimetastatic effect.Not reportedNot mentioned2.5Blood proteaseRadioactivity measured with a gamma counterIntravenous injection of labelled peptide in C57BL/6 micein vivoNoneNoneAt 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50%
1718
105440052001
YIGSR
PVP6,000 -YIGSR5Addition of Polyvinyl pyrrolidone(PVP6,000)FreeLinearLNoneCore sequence located at the β-1 chain of lamininAntimetastatic effect.Not reportedNot mentioned14.5Blood proteaseRadioactivity measured with a gamma counterIntravenous injection of labelled peptide in C57BL/6 micein vivoNoneNoneAt 0.015μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx.
1724
16971651990
SLRRSSGGRIDRIGAQSGLGCNSFRY
ANP'26FreeFreeCyclicLNoneAtrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported0.17-0.25 MBq1.04Rat blood proteasesRadioimmunoassay and RP-HPLCRat blood plasma (infused into fumoral vein and right carotid artery)in vivoNoneNoneNot given
1725
16971651990
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
Atrial natriuretic peptide (ANP)28FreeFreeCyclic (C7-C23)LNoneAtrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported0.17-0.25 MBq7.81 ± 0.38Kallikrein and Endopeptidase 24.11 in presence of inhibitor PhosphoramidonRadioimmunoassay and RP-HPLCRat blood plasma (infused into fumoral vein and right carotid artery)in vivoNoneNoneNot given
1726
16971651990
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
Atrial natriuretic peptide (ANP)28FreeFreeCyclic (C7-C23)LNoneAtrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported0.17-0.25 MBq2.51 ±0.25Kallikrein and Endopeptidase 24.11 in presence of inhibitor AprotininRadioimmunoassay and RP-HPLCRat blood plasma (infused into fumoral vein and right carotid artery)in vivoNoneNoneNot given
1727
16971651990
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
Atrial natriuretic peptide (ANP)28FreeFreeCyclic (C7-C23)LNoneAtrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported0.17-0.25 MBq15.2 ± 1.01Kallikrein and Endopeptidase 24.11 in presence of inhibitors phosphoramidon and aprotinin bothRadioimmunoassay and RP-HPLCRat blood plasma (infused into fumoral vein and right carotid artery)in vivoNoneNoneNot given
1728
19392591991
APRLRFYSL
α-bag cell peptide α-BCP(1-9)9FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide26Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1729
19392591991
APRLRFYSL
α-bag cell peptide α-BCP(1-9)9FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-6 M conc. of peptide35Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1731
19392591991
APRLRFYS
α-BCP(1-8)8FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide27Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1732
19392591991
APRLRF
α-BCP(1-6)6FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide11Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1733
19392591991
APRLR
α-BCP(1-5)5FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide16Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1734
19392591991
RLRFYSL
α-BCP(3-9)7FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide2.1Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1735
19392591991
RLRFYSL
α-BCP(3-9)7FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-6 M conc. of peptide2.7Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1736
19392591991
LRFYSL
α-BCP(4-9)6FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide2.7Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1737
19392591991
RFYSL
α-BCP(5-9)5FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide1.5Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1739
19392591991
YSL
α-BCP(7-9)3FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide9.7Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1740
19392591991
RLRFYS
α-BCP(3-8)6FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide1.5Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1741
19392591991
LRFYS
α-BCP(4-8)5FreeFreeLinearLNoneBag cells in the abdominal ganglion of the marine snail AplysiaNeurotransmitterNot reported10-5 M conc. of peptide1.5Aplysia haemolymph proteasesHPLCHeamolymph of Aplysiain vitroNoneNoneNot given
1743
157690922005
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLNoneProglucagon moleculeGlucose-dependent insulinotropic effectNot reported10 µg/kg9.09Rat blood proteasesELISARat blood plasma (Subcutaneous Injection)in vivoNoneNone100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose
1744
157690922005
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
PEG2k-Lys-GLP-130FreeAmidationLinearLPegylation at LysineProglucagon moleculeGlucose-dependent insulinotropic effectNot reported10 µg/kg21.67Rat blood proteasesELISARat blood plasma (Subcutaneous Injection)in vivoNoneNone100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose
1745
157690922005
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLNoneProglucagon moleculeGlucose-dependent insulinotropic effectNot reported1 µg/kg2.61Rat blood proteasesELISARat blood plasma (Intravenous injection)in vivoNoneNone100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose
1746
157690922005
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
PEG2k-Lys-GLP-130FreeAmidationLinearLPegylation at LysineProglucagon moleculeGlucose-dependent insulinotropic effectNot reported1 µg/kg33.36Rat blood proteasesELISARat blood plasma (Intravenous injection)in vivoNoneNone100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose
1747
158821442005
DNPSLSIDLTFHLLRTLLELARTQSQRERAEQNRIIFDSV
Ucn1 (urocortin 1)40FreeFreeLinearLNoneUrocortin 1Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetiteNot reported50 μg54 ±3Human blood proteasesNot mentionedHuman blood plasma(Male patients with stable congestive heart failure) (Intravenous injection)in vivoNoneNoneNot given
1748
158821442005
DNPSLSIDLTFHLLRTLLELARTQSQRERAEQNRIIFDSV
Ucn1 (urocortin 1)40FreeFreeLinearLNoneUrocortin 1Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetiteNot reported50 μg52 ±3Human blood proteasesNot mentionedHuman blood plasma (Normal humans) (Intravenous)in vivoNoneNoneNot given
1749
160999412005
ELRMSSSYPTGLADVKAGPAQTLIRPQDMKGASRSPEDSSPDAARIRV
proADM 45 €“92 (Adrenomedullin)48FreeFreeLinearLNoneSynthetically synthesised proADM 45 €“92Vasodilatory peptideNot reported0.29nmol/L22Human blood proteasesSandwich immunoluminometric AssayHuman blood plasmain vitroNoneNoneNot given
1750
164768512014
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNoneB-type cardiac natriuretic peptidesVasodilatorNot reportedNot mentioned5.6 ±0.45Human blood proteasesNot mentionedHuman plasma of patients with mild, stable heart failurein vivoNoneNoneNot given
1751
164768512014
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNoneB-type cardiac natriuretic peptidesVasodilatorNot reportedNot mentioned11 ±1.3Human blood proteasesNot mentionedHuman plasma of patients with mild, stable heart failure given infusion of metoprololin vivoNoneNoneNot given
1752
164768512014
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNoneB-type cardiac natriuretic peptidesVasodilatorNot reportedNot mentioned5.7 ±0.8Human blood proteasesNot mentionedHuman plasma (Normal humans)in vivoNoneNoneNot given
1753
164768512014
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNoneB-type cardiac natriuretic peptidesVasodilatorNot reportedNot mentioned6.6 ±1.3Human blood proteasesNot mentionedHuman plasma (Normal humans given infusion of metoprolol)in vivoNoneNoneNot given
1757
164727502006
TVPVDLASRQEEEEQSPDSTEQEPVTLPR
E2-PESTE304Q29FreeFreeLinearLNoneE2 protein from papillomavirusGene transcriptionNot reportedNot mentioned24Not mentionedPulse chase experimentpMEP-E2 CV-1 cell linesin vitro15014086NoneNot mentioned
1759
165860642006
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP130FreeAmidationLinearLNoneSynthetically synthesized Glucagon-like peptide-1InsulinotropicNot reportedNot mentioned6 ±0.5Rat liver proteasesRP-HPLCRat liver homogenatein vitro16505481None380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1760
165860642006
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP130FreeAmidationLinearLNoneSynthetically synthesized Glucagon-like peptide-1InsulinotropicNot reportedNot mentioned1 ±0.2Rat kidney proteasesRP-HPLCRat kidney homogenatein vitro16505481None380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1763
165860642006
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-PEG/GLP-130FreeAmidationLinearLPegylation at N terminus His7Synthetically synthesized Glucagon-like peptide-1 analoguesInsulinotropicNot reportedNot mentioned23 ±7Rat kidney proteasesRP-HPLCRat kidney homogenatein vitro16505481None290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1766
165860642006
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Lys-PEG/GLP-130FreeAmidationLinearLPegylation on Lys34Synthetically synthesized Glucagon-like peptide-1 analoguesInsulinotropicNot reportedNot mentioned28 ±1Rat kidney proteasesRP-HPLCRat kidney homogenatein vitro16505481None150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l])
1774
169905572006
CNGRCGGK
cNGR8AcetylationAmidationCyclicLNoneSynthetic peptideTargets CD13/APN which is present on angiogenic vessels so used for molecular imagingNot reported0.75μg/g15.4 ±3.4Mouse plasma proteasesFluorometeryMouse plasma of Murine myocardial infarction (MI) modelin vivoNoneNoneNot given
1776
173746602007
IPP
IPP3FreeFreeLinearLNoneLactotripeptideACE(Angeotensin converting enzyme)-inhibiting peptideNot reportedNot mentioned~ 30Pancreatic proteasesRP-HPLCHuman blood plasma (oral)in vivoNoneNoneNot given
1777
174792562007
SLRRSSCFGGRIDRIGAQSGCNSFRY
ANP26FreeFreeLinearLNoneSynthetic peptideAtrial natriuratic peptideNot reported0.05 μg/kg per minute2.4 ±0.7Human blood proteasesRadioimmunoassayHuman blood plasmain vitroNoneNoneNot given
1778
174792562007
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNoneSynthetic peptideVasodilatorNot reported0.01 μg/kg per minute12.1 ±3.0Human blood proteasesRadioimmunoassayHuman blood plasmain vitroNoneNoneNot given
1791
176408992007
MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
T-65136FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg0.3Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.008 µg/ml against IIIB virus
1792
176408992007
MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
T-65136FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg0.3Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.033 µg/ml against 098 virus
1793
176408992007
MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
T-65136FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg0.3Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.060 µg/ml against 098-T20 virus
1794
176408992007
MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
T-65136FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg0.3Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.151 µg/ml against 098-T1249 virus virus
1795
176408992007
MTWMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
T-65136FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg0.3Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=7.599 µg/ml against 098-T651 virus
1869
180857212007
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeFreeLinearLNoneGlucagonCounter-regulatory hormoneNot reportedNot mentioned~2DPP-IVELISAMouse plasmain vivoNoneNoneNot given
1870
183073132007
R-X-R
CAP 12FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 83 µM for S.aureus
1871
183073132007
R-X-R
CAP 12FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 50 µM for Methicillin- resistant S.aureus
1872
183073132007
R-X-R
CAP 12FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 25 µM for Methicillin- resistant S.epidermis
1882
183073132007
R-X-R
CAP 52FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 11 µM for S.aureus
1883
183073132007
R-X-R
CAP 52FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 9 µM for Methicillin- resistant S.aureus
1884
183073132007
R-X-R
CAP 52FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 6 µM for Methicillin- resistant S.epidermis
1885
183073132007
R-X-R
CAP 62FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 14 µM for S.aureus
1886
183073132007
R-X-R
CAP 62FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 9 µM for Methicillin- resistant S.aureus
1887
183073132007
R-X-R
CAP 62FreeNHBnLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL1TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 6 µM for Methicillin- resistant S.epidermis
1933
183073132007
R-X-R
CAP 192FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 29 µM for S.aureus
1934
183073132007
R-X-R
CAP 192FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 29 µM for Methicillin- resistant S.aureus
1935
183073132007
R-X-R
CAP 192FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 20 µM for Methicillin- resistant S.epidermis
1936
183073132007
R-Bip-R
CAP 192AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 29 µM for S.aureus
1937
183073132007
R-Bip-R
CAP 192AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 29 µM for Methicillin- resistant S.aureus
1938
183073132007
R-Bip-R
CAP 192AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 20 µM for Methicillin- resistant S.epidermis
1939
183073132007
R-X-R
CAP 202FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 50 µM for S.aureus
1940
183073132007
R-X-R
CAP 202FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 50 µM for Methicillin- resistant S.aureus
1941
183073132007
R-X-R
CAP 202FreeCH2CH2PhLinearLX= structure given in paperSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 10 µM for Methicillin- resistant S.epidermis
1942
183073132007
R-Bip-R
CAP 202AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 50 µM for S.aureus
1943
183073132007
R-Bip-R
CAP 202AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 50 µM for Methicillin- resistant S.aureus
1944
183073132007
R-Bip-R
CAP 202AcetylationY= structure given in paperLinearLBipSynthetic peptideAntimicrobialNot reported1 mg/mL0.6TrypsinRP-HPLCTrypsinin vitroNoneNoneMIC= 10 µM for Methicillin- resistant S.epidermis
1962
184818522008
((POG)5 (PQGPGGPPG) (POG)5)3
3A117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned580Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1963
184818522008
((POG)5 (PQGPGSPPG) (POG)5)3
3A'117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned910Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1964
184818522008
((POG)5 (PVGAAGATG) (POG)5)3
3B117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned345Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1965
184818522008
((POG)5 (PVGAASATG) (POG)5)3
3B'117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned655Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1966
184818522008
(POG)5 (PQGPGGPPG) (POG)5 (PKG)5 (PQGPGGPPG) (PKG)5 (DOG)5 (PVGAAGATG) (DOG)5
A.A.B117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned190Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1967
184818522008
(POG)5 (PQGPGGPPG) (POG)5 (PKG)5 (PQGPGGPPG) (PKG)5 (DOG)5 (PVGAAGATG) (DOG)6
A.A.B'117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned300Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1968
184818522008
(POG)5 (PQGPGSPPG) (POG)5 (PKG)5 (PQGPGSPPG) (PKG)5 (PKG)5 (PQGPGSPPG) (PKG)5
A'.A'.B117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned325Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1969
184818522008
(POG)5 (PQGPGSPPG) (POG)5 (PKG)5 (PQGPGSPPG) (PKG)5 (POG)5 (PVGAASATG) (POG)5
A'.A'.B'117AcetylationAmidationLinearLNoneSynthetic Collagen peptideStructural component of connective tissuesNot reportedNot mentioned470Not mentionedHPLC and MALDI-TOFNot reportedin vitroNoneNoneNot available
1970
185530942008
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNonePro-Brain natriuretic peptideVasodilatorNot reportedNot mentioned~22Human blood proteasesELISAHuman plasmain vitroNoneNoneNot available
1974
192234222009
SPRGDLAVLGHKY
HBP-113FreeFreeLinearLNoneSynthetic peptideNot mentionedNot reportedNot mentioned55Not mentionedHPLCHuman serumin vitroNoneNoneIC50=38.9nM
1975
194030442008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1/Fc30FreeAmidationLinearLNoneProglucagon moleculeAntidiabeticNot reported16nM~20Rabbit serum proteasesLuciferase reporter assayRabbit serumex vivoNoneNoneNot available
1976
194030442008
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLNoneProglucagon moleculeAntidiabeticNot reported0.4nM<5Rabbit serum proteasesLuciferase reporter assayRabbit serumex vivoNoneNoneNot available
1977
194133092009
IRRADRAAVPGGGGRGD
HM317FreeFreeLinearLNoneRGD- modified endostatin derived peptideAntitumorNot reported1mg/ml27.66 ± 7.37Rat blood proteasesRP-HPLCRat blood serum (Intravenous injection)in vivoNoneNoneLess active in the inhibition of angiogenesis in the chorioallantoic membrane of chick embryos
1979
194580862009
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP28FreeFreeCyclic (C7-C23)LNoneC terminus of atrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported1 µM2.6Human kidney membrane proteasesRadioimmunoassayHuman kidney membranesin vitroNoneNoneIC50=2.4nM
1980
194580862009
SLRRSSCFGGRMDRIGAQSGLGCNSFRYRITAREDKQGWA
fsANP40FreeFreeCyclic (C7-C23)LNoneC terminus of atrial natriuretic peptideNatriuretic, diuretic and vasorelaxantNot reported1 µM4.5Human kidney membrane proteasesRadioimmunoassayHuman kidney membranesin vitroNoneNoneIC50=3.2nM
1981
195310532009
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLNoneProglucagon moleculeAntidiabeticNot reportedNot mentioned20DPP IVELISAMice (Subcutaneous injection)in vivoNoneNoneNot available
1983
195529232011
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLNoneProglucagon moleculeInsulinomimetic and insulinotropicNot reported27.9 ± 5.8 μg/ml1 to 2Rabbit blood proteasesELISARabbit bloodin vivoNoneNoneNot available
1984
195726362009
NISHTKEKKKGKAKKKRLTK
N-WASP181-20020FreeFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported1 mg/mL6.7Not mentionedHPLCRat renal brush border membrane suspensionin vitroNoneNoneIC50=0.041 mM with gentamicin
1985
195726362009
NISHTKEKKKGKAKKKRLTK
PEG1k-N-W20PegylationFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported100 µg/mL12.9Not mentionedHPLCRat renal brush border membrane suspensionin vitroNoneNoneIC50=0.128 mM with gentamicin
1986
195726362009
NISHTKEKKKGKAKKKRLTK
N-WASP181-20020FreeFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported100 µg/mL6.7Not mentionedHPLCRat renal brush border membrane suspensionin vitroNoneNoneIC50=46.1 mg/kg with Arbekacin
1987
195726362009
NISHTKEKKKGKAKKKRLTK
N-WASP181-20020FreeFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported100mg/kg2.7Not mentionedHPLCRat blood plasma (Intravenous)in vivoNoneNoneIC50=46.1 mg/kg with Arbekacin
1988
195726362009
NISHTKEKKKGKAKKKRLTK
PEG1k-N-W20PegylationFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported100mg/kg4.6Not mentionedHPLCRat blood plasma (Intravenous)in vivoNoneNoneIC50=17.8 mg/kg with Arbekacin
1989
195726362009
NISHTKEKKKGKAKKKRLTK
PEG1k-N-W20PegylationFreeLinearLNoneSynthetic peptideInhibits renal accumulation of aminoglycoside antibioticsNot reported100 µg/mL12.9Not mentionedHPLCRat renal brush border membrane suspensionin vitroNoneNoneIC50=17.8 mg/kg with Arbekacin
2001
119627212001
DIRCKDDEFTHLYTLIVRPDNTYEVKIDNSQVESGSLEDDWDFLPPKKIKDPDAAKPEDWDERAKIDDPTDSKPEDWDKPEHIPDPDAKKPEDWDEEMDGEWEPPVIQNPEYKGEWKPRQIDNP
CTR-S domain124FreeFreeLinearLNoneCTR (Calreticulin)It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathwayNot reportedNot mentioned1.21 ± 0.34 in distribution phaseSerine ProteasesRadioactivity measured with a gamma counterRat plasmain vivoNoneNoneBiological activity =2 m Ci/nmol
2002
119627212001
DIRCKDDEFTHLYTLIVRPDNTYEVKIDNSQVESGSLEDDWDFLPPKKIKDPDAAKPEDWDERAKIDDPTDSKPEDWDKPEHIPDPDAKKPEDWDEEMDGEWEPPVIQNPEYKGEWKPRQIDNP
CTR-S domain124FreeFreeLinearLNoneCTR (Calreticulin)It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathwayNot reportedNot mentioned40.5 ± 2.7 in elimination phaseSerine ProteasesRadioactivity measured with a gamma counterRat plasmain vivoNoneNoneBiological activity =2 m Ci/nmol
2003
119767972002
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeAmidationLinearLRadiolabelling of GLP-1by [123I]Proglucagon moleculeAntidiabeticNot reported10 MBq of the radiolabelled peptides7.0 ±2.1 for É‘ phaseRat blood proteasesScintigraphyNEDH Rats (rat tumour model)in vivoNoneNoneNot mentioned
2005
119767972002
HSDGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exendin 339FreeFreeLinearLRadiolabelling of exendin 3 at position 1 (histidine)Heloderma horridum venomGLP-1 agonistNot reported10 MBq of the radiolabelled peptides13 ±3.2Rat blood proteasesScintigraphyNEDH Rats (rat tumour model)in vivoNoneNoneNot mentioned
2007
155879342004
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Human BNP32FreeFreeLinearLNoneB-type cardiac natriuretic peptidesVasodilatorNot reportedNot mentioned3.1Not mentionedEIAMice plasma (Intravenous injection)in vivoNoneNoneEC50 =0.46 ± 1.1 nM
2011
172924922007
NPMYNAVSNADLMDFKNLLDHLEEKMPLEDEVVPPQVLSEPNEEAGAALSPLPEVPPWTGEVSPAQRDGGALGRGPWDSSDRSALLKSKLRALLTAPR
NT-ANP98FreeFreeLinearLNoneANP (A- type natriuretic peptide)Natriuretic, diuretic and vasorelaxantNot reported650fmol/ml1Human blood proteasesRadioimmunoassayHuman bloodin vitroNoneNoneNot mentioned
2012
183535072008
HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK
PACAP3838FreeAmidationLinearLNoneSynthetically synthesised pituitary adenylate cyclase-activating polypeptideTherapeutic Neuropeptide for neurodegenerative diseases.Not reported10-5 M23 ±6DPP IVRP-HPLC and MS-MALDI-TOFDPP IVin vitroNoneNoneIC50 = 7.7 ±1.4 nM
2013
183535072008
HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK
PACAP3838FreeAmidationLinearLNoneSynthetically synthesised pituitary adenylate cyclase-activating polypeptideTherapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M4.3 ±0.3Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 7.7 ±1.4 nM
2018
183535072008
HSDGIFTDSYSRYRKQMAVKKYLAAVLGKRYKQRVKNK
[ψCH2-NH21-22]PACAP3838FreeAmidationLinearL[ψCH2-NH21-22]Synthetic analog of PACAP38Therapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M18 ±2Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 59 ±17 nM
2019
183535072008
HSDGIFTDSYSRYRKQMAVAKYLAAVLGKRYKQRVKNK
[Ala20]PACAP3838FreeAmidationLinearLNoneSynthetic analog of PACAP38Therapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M8.3 ±1.2Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 1.2 ±0.4 nM
2020
183535072008
HSDGIFTDSYSRYRKQMAVKAYLAAVLGKRYKQRVKNK
[Ala21]PACAP3838FreeAmidationLinearLNoneSynthetic analog of PACAP38Therapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M6.6 ±0.5Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 2.0 ±0.5 nM
2024
183535072008
HSDGIFTDSYSRYAKQMAVAKYLAAVLGKRYKQRVKNK
Acetyl-[Ala14, Ala20]PACAP38-propylamide38AcetylationPropylamidationLinearLNoneSynthetic analog of PACAP38Therapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M15 ±2Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 5.3 ±1.7 nM
2026
183535072008
HSDGIFTDSYSRYRAQMAVAKYLAAVLGKRYKQRVKNK
Acetyl-[Ala15, Ala20]PACAP38-propylamide38AcetylationPropylamidationLinearLNoneSynthetic analog of PACAP38Therapeutic Neuropeptide for neurodegenerative diseases.Not reported10-4 M25 ±2Human plasma proteasesRP-HPLC and MS-MALDI-TOFHuman plasmain vitroNoneNoneIC50 = 1.8 ±0.7 nM
2027
183535072008
HSDGIFTDSYSRYRKQMAVKKYLAAVL
PACAP2727FreeAmidationLinearLNoneSynthetically synthesised pituitary adenylate cyclase-activating polypeptideTherapeutic Neuropeptide for neurodegenerative diseases.Not reported10-5 M39 ±4DPP IVRP-HPLC and MS-MALDI-TOFDPP IVin vitroNoneNoneIC50 = 9.6 ±2.4 nM
2037
190417162009
AGCKNFFWKTFTSC
SST (Somatostatin)14FreeFreeCyclic (C3-C14)LNoneSomatostatinNeurotransmitterNot reported1.8 mg/ml7.6Rat blood proteasesELISARat plasma (Intravenous injection)in vivoNoneNoneNot available
2038
190417162009
AGCKNFFWKTFTSC
LCNP/SST (Somatostatin adsorbed on Liquid crystalline nanoparticles for 10 min)14FreeFreeCyclic (C3-C14)LNoneSomatostatin adsorbed on Liquid crystalline nanoparticlesNeurotransmitterNot reported1.8 mg/ml0.73 ±0.03Rat blood proteasesELISARat plasma (Intravenous injection)in vivoNoneNoneNot available
2039
190417162009
AGCKNFFWKTFTSC
LCNP/SST (Somatostatin adsorbed on Liquid crystalline nanoparticles for 18 hours)14FreeFreeCyclic (C3-C14)LNoneSomatostatin adsorbed on Liquid crystalline nanoparticlesNeurotransmitterNot reported1.8 mg/ml0.79 ±0.17Rat blood proteasesELISARat plasma (Intravenous injection)in vivoNoneNoneNot available
2052
198361832010
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP32FreeFreeLinearLNonePorcine brainVasodilatorNot reported31.2ng/ml3.1Mouse plasma proteasesELISAMouse plasmain vivoNoneNoneNot mentioned
2053
213297332011
L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]
Octreotide acetate8FreeFreeCyclic (C2-C7)Mix2-hydroxy-1-(hydroxymethyl)Synthetic analog of SomatostatinUsed for treatment of acromegalyNot reported30μg/100μl52.1Mouse blood proteasesEIAMice blood serum (oral delivery in 0.5% Intravail)in vivoNoneNoneNot mentioned
2054
213297332011
L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]
Octreotide acetate8FreeFreeCyclic (C2-C7)Mix2-hydroxy-1-(hydroxymethyl)Synthetic analog of SomatostatinUsed for treatment of acromegalyNot reported30μg/100μl25.8Mouse blood proteasesEIAMice blood serum (oral delivery in 1.5% Intravail)in vivoNoneNoneNot mentioned
2055
213297332011
L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]
Octreotide acetate8FreeFreeCyclic (C2-C7)Mix2-hydroxy-1-(hydroxymethyl)Synthetic analog of SomatostatinUsed for treatment of acromegalyNot reported30μg/100μl23.6Mouse blood proteasesEIAMice blood serum (oral delivery in 3.0% Intravail)in vivoNoneNoneNot mentioned
2056
213297332011
L-Cysteinamide, D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-Lthreonyl-N-[2-hydroxy-1-(hydroxymethyl)propyl]
Octreotide acetate8FreeFreeCyclic (C2-C7)Mix2-hydroxy-1-(hydroxymethyl)Synthetic analog of SomatostatinUsed for treatment of acromegalyNot reported30μg/100μl1.3Mouse blood proteasesEIAMice blood serum (Subcutaneous injection)in vivoNoneNoneNot mentioned
2062
229346812012
YaG-MePhe-G
DAMGO5FreeFreeLinearMixMethylation at phenylalanineSynthetic peptideOpioid peptideNot reported5.0 mg/kg9.2 ± 2.1Rat blood proteasesESI-LC ˆ’MS/MSRat blood plasma (Intravenous)in vivoNoneNoneNot mentioned
2068
238360302013
MAPRGFSCLLLLTGEIDLPVKRRA
HNG ( substitution at position 14 (Gly for Ser) in HN seq)24FreeFreeLinearLNoneSynthetic peptideCytoprotectiveNot reported16 fold higher than original concentration~30Mouse plasma proteasesELISAMice plasmain vitro15655255NoneNot available
2069
243784402013
YRWYGYTPQNVIGGGKLlLKlLkkLLKlLKKK
EGFR2R-lytic peptide32FreeFreeLinearMixNoneSynthetic peptideCytotoxic and antitumorNot reportedNot mentioned9.4 ± 1.5Not mentionedNot mentionedBovine serumin vivoNoneNoneNot available
2070
243784402013
YRWYGYTPQNVIGGGKLlLKlLkkLLKlLKKK
EGFR2R-lytic peptide-gelatin complex32FreeFreeLinearMixNoneSynthetic peptideCytotoxic and antitumorNot reportedNot mentioned19.3 ±2.9Not mentionedNot mentionedBovine serumin vivoNoneNoneNot available
2071
33486031987
N-MeVal-EtPro-N-MeThr-Leu-MePro-AMHA-Pro-N-MeLeu- Gly
DihydromycoplanecinA (DHMP A)10alpha-hydroxybutyric acidFreeCyclicLN-MeVal; N-methylvaline, EtPro; Ethylproline, N-MeThr; N-methylthreonine MePro; Methylproline, AMHA; 2-amino-5-methylhexanoic acid, N-MeLeu; N-methylleucineActive metabolite in urine of mice and dogsAntibioticNot reported10 mg/kg0.5Mouse blood proteasesNot mentionedMice serum (Intravenous)in vivoNoneNoneLD50>6000mg/kg administered orally to mice
2074
61175061981
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive Intestinal Peptide28FreeAmidationLinearLNonePorcine vasoactive intestinal peptideVasoactive intestinal peptideNot reported103.7 ± 14.8 ml/kg1.80 ± 0.1Dog blood proteasesRadioimmunoassayDog plasma (Intravenous)in vivoNoneNone150-220 µci/ µg
2075
81811152014
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial natriuretic factor (ANF)28FreeFreeLinearLNoneCardiac atriaPeptide hormoneNot reportedNot mentioned2.5Human blood proteasesRadioimmunoassayHuman blood plasmain vitroNoneNoneNot available
2076
84066702014
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial natriuretic factor (ANF)28FreeFreeLinearLNoneCardiac atrium in response to myocardial stretchPeptide hormoneNot reportedNot mentioned20 to 180Human blood proteasesRadioimmunoassayHuman blood plasmain vitroNoneNoneNot available
2077
89104261996
KPTFRRLKWK
LL:36 €“4510FreeFreeLinearLNoneAnalogue of Limulus anti-lipopolysaccharide factorAntibacterialNot reported2.5 µg/ml17Proteases present in fetal calf serumRP-HPLCFetal calf serumin vitroNoneNoneNo cell lysis done by this peptide
2080
90672971996
YGGFLRRl
E-2078 [N-methyl-Tyr1, N-methyl-Arg7-D-Leu8] Dyn A (1 €“8) ethylamide]N.A.MethylationEthylamideLinearMixMethylation on Arg7 and Tyr1Dynorphin A (1 €“ 8) analogAnalgesicNot reported10 mg/kg44Monkey blood proteasesMALDI-MSRhesus monkey blood plasma (Intravenous)in vivo7479294NoneNot available
2081
204189552010
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNonePancreasPlays a major regulatory role in controlling hypoglycemiaNot reportedNot mentioned<10Human blood proteasesELISAHuman serumin vitroNoneNoneNot available
2083
N.A.2004
AAGIGILTV
Melan-A27-359FreeFreeLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM5Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 4 nM
2084
N.A.2004
EAAGIGILTV
Melan-A26-3510FreeFreeLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM45Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 0.25 nM
2085
N.A.2004
ELAGIGILTV
Melan-A26-35 A27L10FreeFreeLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM40Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 0.01 nM
2107
N.A.2011
FVPIFTYGELQRMQEKERNKGQ
Motilin22FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg3.26Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2108
N.A.2011
FVPIFTYGELQRSPEHQRVQQRKESKKPPAKLQPR
Chimeric Motilin A35FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.74Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2109
N.A.2011
FVPIFTYGELQREHQRVQQQRKESKKPPAKLQPR
Chimeric Motilin B34FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.14Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2110
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Chimeric Motilin C31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg8.9 ±0.53Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2111
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Chimeric Motilin D31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg8.9 ±0.50Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2112
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Chimeric Motilin E31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg8.03Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2113
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Chimeric Motilin F31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.37Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2114
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAKLQPR
Chimeric Motilin G31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.25Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2115
N.A.2011
FVPIFTYGELQRVQQRKESKKPPAKLQ
Chimeric Motilin H27FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg10.43Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2116
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPPAK
Chimeric Motilin I27FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.76Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2117
N.A.2011
FVPIFTYGELQRQRVQQRKESKKPP
Chimeric Motilin J25FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg6.34Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2118
N.A.2011
FVPIFTYGELQRQRVQQRKESKK
Chimeric Motilin K23FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg6.14Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2119
N.A.2011
FVPIFTYGELQRQRVQQRKES
Chimeric Motilin L21FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg4.89Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2120
N.A.2011
FVPIFTYGELQRQRVQQRK
Chimeric Motilin M19FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg2.39Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2121
N.A.2011
FVPIFTYGELQRVQQRKEKKPPAKLQPR
Chimeric Motilin N28FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.12Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2122
N.A.2011
FVPIFTYGELQRVQQRKEFKKPPAKLQPR
Chimeric Motilin O29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg7.73Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2123
N.A.2011
FVPIFTYGELQRVQQRKETKKPPAKLQPR
Chimeric Motilin P29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.67Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2124
N.A.2011
FVPIFTYGELQRVQQRKEPKKPPAKLQPR
Chimeric Motilin Q29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.65Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2125
N.A.2011
FVPIFTYGELQRVQQRKELKKPPAKLQPR
Chimeric Motilin R29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.13Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2126
N.A.2011
FVPIFTYGELQRVQQRKEAKKPPAKLQPR
Chimeric Motilin S29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.29Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2127
N.A.2011
FVPIFTYGELORVQQRKNSKKPPAKLQPR
Chimeric Motilin T29FreeFreeLinearLOrnithineMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.47Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2128
N.A.2011
FVPIFTYGELQRVQQRKQSKKPPAKLQPR
Chimeric Motilin U29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.66Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2129
N.A.2011
FVPIFTYGELQRVQQRKDSKKPPAKLQPR
Chimeric Motilin V29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg10.14Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2130
N.A.2011
FVPIFTYGELQRVQQRKKKPPAKLQPR
Chimeric Motilin W27FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.39Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2131
N.A.2011
FVPIFTYGELQRVQQKRDSRRPPAKLQPR
Chimeric Motilin X29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg7.89Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2132
N.A.2011
FVPIFTYGELQRVQQKKSEKRPPAKLQPR
Chimeric Motilin Y29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.6Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2133
N.A.2011
FVPIFTYGELQRVQQRKGESKKPPAKLQPR
Chimeric Motilin Z30FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg10.53Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2134
N.A.2011
FVPIFTYGELQRQQRKESGKKPPAKLQPR
Chimeric Motilin-i29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.55Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2135
N.A.2011
FVPIFTYGELQRVQQRKGGESKKPPAKLQPR
Chimeric Motilin-ii31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.5Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2136
N.A.2011
FVPIFTYGELQRVQQRKGGESKKPPAKLQPR
Chimeric Motilin-iii31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg10.65Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2137
N.A.2011
FVPIFTYGELQRVQQRKESKKAKLQPR
Chimeric Motilin-iv27FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg7.73Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2138
N.A.2011
FVPIFTYGELQRVQQRKESKKAKLAALKA
Chimeric Motilin-v29FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg8.94Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2139
N.A.2011
FVPIFTYGELQRVQQRKESKKPPAKLAALKA
Chimeric Motilin-vi31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg9.94Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2140
N.A.2011
FVPIFTYGELQRVQQRKESKKPPAELAALEA
Chimeric Motilin-vii31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg12.78Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2141
N.A.2011
FVPIFTYGELQRVQQRKESKKPPAELAALKA
Chimeric Motilin-viii31FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg11.56Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2142
N.A.2011
FVPIFTYGELQRVQQRKESKKMITIR
Chimeric Motilin-ix26FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg4.39Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2143
N.A.2011
FVPIFTYGELQRVQQRKESKKPPMITIR
Chimeric Motilin-x28FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg5.25Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2144
N.A.2011
FVPIFTYGELQRKESKKPAKLAALKA
Chimeric Motilin-xi26FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg10.29Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2145
N.A.2011
FVPIFTYGELQRVQQKKAYSPDKERKPPALQPR
Chimeric Motilin-xii33FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg13.03Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2146
N.A.2011
FVPIFTYGELQRVQQKKAYSPDKERKPPAKLQPR
Chimeric Motilin-xiii34FreeFreeLinearLNoneMotilinRegulator of motility of digestive tractN.A.10 nM/ Kg13.09Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2147
N.A.2011
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg2.88Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2148
N.A.2011
CFGGRMDRIGAQSGLGCNSFRYVQQRKESKKPPAKLQPR
Chimeric ANP-A39FreeFreeCyclic (C1-C17)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg24Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2149
N.A.2011
VQQRKESKKPPAKLQPRCFGGRMDRIGAQSGLGCNSFRY
Chimeric ANP-B39FreeFreeCyclic (C18-C34)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg40Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2150
N.A.2011
RPQLKAPPKKSEKRQQVCFGGRMDRIGAQSGLGCNSFRY
Chimeric ANP-C39FreeFreeCyclic (C18-C34)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg27.2Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2151
N.A.2011
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg11.2Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2152
N.A.2011
CFGGRMDRIGAQSGLGCNSFRYVQQRKESKKPPAKLQPR
Chimeric ANP-A39FreeFreeCyclic (C1-C17)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg46.4Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2153
N.A.2011
VQQRKESKKPPAKLQPRCFGGRMDRIGAQSGLGCNSFRY
Chimeric ANP-B39FreeFreeCyclic (C18-C34)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg57.3Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2154
N.A.2011
RPQLKAPPKKSEKRQQVCFGGRMDRIGAQSGLGCNSFRY
Chimeric ANP-C39FreeFreeCyclic (C18-C34)LNoneANP (Atrial natriuretic peptide)Regulator of sodium ions in heartN.A.0.1 mg/ Kg37.8Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2155
N.A.2011
GLSKGCFGLKLDRIGSMSGLGC
CNP-22 (C-type natriuretic peptide)22FreeFreeCyclic (C6-C22)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.0.1 mg/ Kg7.8Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2156
N.A.2011
RPQLKAPPKKSEKRQQVCFGLKLDRIGSMSGLGC
Chimeric CNP-A34FreeFreeCyclic (C18-C34)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.0.1 mg/ Kg20.7Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2157
N.A.2011
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Chimeric CNP-B34FreeFreeCyclic (C1-C17)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.0.1 mg/ Kg24Not mentionedCompetitive RadioimmunoassayRat plasma (Subcutaneous)in vivoNoneEP2277890A1Not mentioned
2158
N.A.2011
GLSKGCFGLKLDRIGSMSGLGC
CNP-22 (C-type natriuretic peptide)22FreeFreeCyclic (C6-C22)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.0.1 mg/ Kg2.93Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2159
N.A.2011
RPQLKAPPKKSEKRQQVCFGLKLDRIGSMSGLGC
Chimeric CNP-A34FreeFreeCyclic (C18-C34)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.0.1 mg/ Kg21.7Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2161
N.A.2011
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Chimeric CNP-C34FreeFreeCyclic (C1-C17)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg15.03Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2162
N.A.2011
GLSKGFGLKLDRISMSGLGCVQQRKESKKPPAKLQPR
Chimeric CNP-D37FreeFreeCyclic (C6-C22)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg20.3Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2163
N.A.2011
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPRESKKPPAKLQPR
Chimeric CNP-E46FreeFreeCyclic (C1-C17)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg18.4Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2164
N.A.2011
RPQLKAPPKKSEKRQQVCFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Chimeric CNP-F51FreeFreeCyclic (C18-C34)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg17.38Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2165
N.A.2011
VQQRKESKKPPAKLQPRCFGLKLDRIGSMSGLGC
Chimeric CNP-G34FreeFreeCyclic (C18-C34)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg17.75Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2166
N.A.2011
RPQLKAPPKKSEKRQQVCFGLKLDRIGSMSGLGC
Chimeric CNP-H34FreeFreeCyclic (C18-C34)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg14.86Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2167
N.A.2011
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Chimeric CNP-I34FreeAmidationCyclic (C1-C17)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg14.5Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2168
N.A.2011
GLSKGCFGLKLDRIGSMSGLGCVQQRKDSKKPPAKLQPR
Chimeric CNP-J39FreeFreeCyclic (C6-C22)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.20 nm/ Kg31.24Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2169
N.A.2011
CFGLKLDRIGSMSGLGCAGSVDHKGKQRKWDHPKR
Chimeric CNP-K35FreeFreeCyclic (C1-C17)LNoneCNP-22 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.20 nm/ Kg18.03Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2170
N.A.2011
DLRVDTKSRAAWARLLQEHPNARKYKGANKKGLSKGGLSKGCFGLKLDRIGSMSGLGC
CNP-53 (C-type natriuretic peptide)58FreeFreeCyclic (C42-C58)LNoneCNP-58 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg15.72Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2171
N.A.2011
GLSKGCFGLKLDRIGSMSGLGC
CNP-22 (C-type natriuretic peptide)22FreeFreeCyclic (C6-C22)LNoneCNP-58 (C-type natriuretic peptide)Third member of natriuretic peptide family with multiple functionsN.A.10 nm/ Kg1.11Rat blood proteasesCompetitive RadioimmunoassayRat plasma (Intravenous)in vivoNoneEP2277890A1Not mentioned
2172
N.A.2012
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exendin-439FreeAmidationLinearLNoneVenom of Heloderma horridumInsulinotropic peptideN.A.520 micro g/Kg0.8Not mentionedEIARat plasma (Subcutaneous)in vivoNoneEP2423233A2Blood glucose after 24 hour >25 mM
2175
N.A.2006
HGDGSFSDEMNTILDNLAARDFINWLIQTLITD
Derivative of Glucagon Like Peptide-2 (GLP-2)33FreeAmidationLinearLNoneGLP-2Intestine function modulatorN.A.500 nM/ Kg0.9Not mentionedRadioimmunoassayRat plasma (Subcutaneous)in vivoNoneUS7112567B2Not mentioned
2180
N.A.2009
YGGFLRRIRPK
Modified Dynorphin (1-13)13FreeAddition of hydroxyl groupLinearLNoneDynorphin peptideEndogenous opioid found in CNSN.A.4 mg/ ml10Not mentionedLC/MSplasmain vitroNoneUS 20090175821AlNot mentioned
2181
N.A.2009
YGGFLRRIRPK
Modified Dynorphin(1-13)13FreeAmidationLinearLNoneDynorphin peptideEndogenous opioid found in CNSN.A.4 mg/ ml30Not mentionedLC/MSplasmain vitroNoneUS 20090175821AlNot mentioned
2194
N.A.2012
HVEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
Val8-GLP-1-OH31FreeAddition of hydroxyl groupLinearLNoneGlucagon like peptide1Insulinotropic peptideN.A.10 micro g/ kg0.05Rat blood proteasesRadioimmunoassayRat plasma (Intravenous)in vivoNoneEP1605897B1EC50= 100% (as reference)
2197
N.A.2012
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exendin-439FreeFreeLinearLNoneVenom of Heloderma horridumInsulinotropic peptideN.A.Not mentioned0.7Not mentionedNot mentionedbloodNot mentionedNoneEP2114438B1EC50= 100% (as reference)
2217
153693942004
CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Interferon α2 (IFNα2)146FreeFreeCyclic(C1-C98, C29-138)LGlycosylation at Thr-105IFNα2Antiviral and antiproliferative0-25 hours10 μg/rat in 0.2 mL of PBS~1Rat blood proteasesBIAcore binding assayIntravenously administered to wistar ratsin vivohttp://www.uniprot.org/uniprot/P01563NoneFollowing administration of IFNα2 (100 μg/rat), the circulating antiviral activity declined with a t1/2 value of ˆ¼1 h, reaching a level lower than 20 pM IFNα2, 12 h after administration.
2218
7300722001
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive intestinal peptide28FreeFreeLinearLNonePorcine VIPAntiinflammatory and vasodilatory0 5, 1, 2,3, 4, 5, 6, 7, 8, 9, 10, 12, 15, 20, and 30 minutes0.6, 1.3, and 3.3 pmol/kg/min infused over 30 minutes~1Human blood proteasesRadioimmunoassayIntravenous infusion to humansin vivohttp://www.uniprot.org/uniprot/P01282NoneInfusion of the highest dose of VIP, plasma concentrations of glucose were significantly raised from a basal level of 5.05 ± 0.29 to 5.61 ± 0.27mmol/l. Plasma levels of free fatty acids were increased from 0.40 ± 0.06 to 0.96 ± 0.09 mmol/l
2219
129540662003
ELYENKPRRPYIL
Neurotensin13FreeFreeLinearLNoneBovine hypothalamusInduction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosisNot mentioned1.07mM5.9 ±0.2Rat serum proteaseMALDI-TOF-MSRat serumin vitroNoneNoneBiological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells.
2235
129540662003
ELYENKP-10-RPYIL
KK1613FreeFreeLinearLCOOH-CH(NH2)-CH-CH-CH(NH)-C=NR(H2N) at 8th arginine positionDerivative of Bovine hypothalamusInduction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosisNot mentioned1.07mM14.2 ±0.3Rat serum proteaseMALDI-TOF-MSRat serumin vitroNoneNoneBiological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells.
2236
129540662003
ELYENKP-11-RPYIL
KK1713FreeFreeLinearLCOOH-CH(H2N)CH-CH-CH(HN)-CH(imidazole) at 8th arginine positionDerivative of Bovine hypothalamusInduction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosisNot mentioned1.07mM31.5 ±0.6Rat serum proteaseMALDI-TOF-MSRat serumin vitroNoneNoneBiological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells.
2237
129540662003
ELYENKP-12-RPYIL
KK1813FreeFreeLinearLCOOH-CH(NH2)CH-CH-CH(N-CH-CH-NH-C=NH-CH) at 8th arginine positionDerivative of Bovine hypothalamusInduction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosisNot mentioned1.07mM15.9 ±1.6Rat serum proteaseMALDI-TOF-MSRat serumin vitroNoneNoneBiological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells.
2238
129540662003
ELYENKP-13-RPYIL
KK1913FreeFreeLinearLCOOH-CH(NH2)CH-CH-CH(N-CH-CH-NH-C=NH-CH) at 8th arginine positionDerivative of Bovine hypothalamusInduction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosisNot mentioned1.07mM16.5 ±0.6Rat serum proteaseMALDI-TOF-MSRat serumin vitroNoneNoneBiological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells.
2239
146406802003
ICLKKWPWWPWRRCK
cycloCP-1115FreeAmidationCyclic (C2-C14)LNoneAnalogue of indolicidinAntibacterial0,5,10,20,40,60 minutes50 µg/mL peptide and 0.2 µg/mL trypsin in 100 mM Tris buffer18TrypsinHPLC and MALDI-TOFcycloCP-11 in presence of trypsinin vitroNoneNoneMIC for E.coli=16 µg/ml
2240
146406802003
ILKKWPWWPWRRK
CP1113FreeAmidationLinearLNoneIndolicidin analogueAntibacterial0,5,10,20,40,60 minutes50 µg/mL peptide and 0.2 µg/mL trypsin in 100 mM Tris buffer4TrypsinHPLC and MALDI-TOFCP-11 in presence of trypsinin vitroNoneNoneMIC for E.coli=8 µg/ml
2241
122208902002
CKAFSNSYPYDVPDYASL
Influenza hemagglutinin [(HA) 91 €“108] derivative18AcetylationAmidationLinearLNoneDerivative of B-cell epitope hemagglutinin (HA) 91 €“108 from influenzaModulate immune responseNot mentioned1 mg/ml2Mice lung homogenate proteasesRP-HPLCBALB/c mice lung homogenatein vitroNoneNoneIFN-y production in presence of peptide was measured. Splenocyte was collected after 12 days of immunization, cultured in presence / absence of Inactivated virus(500 HAU/well). Level of IFN-y in presence of virus is ~2500 pg/ml as measured by ELISA.
2243
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M21.2 ±1.1Human blood plasma proteasesTLCHuman plasma mixed with drug Thioridazinein vitroNoneNoneNot mentioned
2244
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M19.6 ±1.0Human blood plasma proteasesTLCHuman plasma mixed with drug Fluphenazinein vitroNoneNoneNot mentioned
2245
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M17.2 ±0.9Human blood plasma proteasesTLCHuman plasma mixed with drug AS-1397in vitroNoneNoneNot mentioned
2246
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M17.1 ±1.0Human blood plasma proteasesTLCHuman plasma mixed with drug Promethazinein vitroNoneNoneNot mentioned
2247
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M17.1 ±1.1Human blood plasma proteasesTLCHuman plasma mixed with drug Chlorpromazinein vitroNoneNoneNot mentioned
2248
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M12.5 ±0.1Human blood plasma proteasesTLCHuman plasma mixed with drug Methotrimeprazinein vitroNoneNoneNot mentioned
2249
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M12.1 ±0.2Human blood plasma proteasesTLCHuman plasma mixed with drug Methotrimeprazinein vitroNoneNoneNot mentioned
2250
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M11.9 ±0.2Human blood plasma proteasesTLCHuman plasma mixed with drug Prochlorperazinein vitroNoneNoneNot mentioned
2251
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M11.4 ±0.3Human blood plasma proteasesTLCHuman plasma mixed with drug Trifluoperazinein vitroNoneNoneNot mentioned
2252
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M12.4 ±0.3Human blood plasma proteasesTLCHuman plasma mixed with drug Molindonein vitroNoneNoneNot mentioned
2253
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M12.4 ±0.4Human blood plasma proteasesTLCHuman plasma mixed with drug Loxapinein vitroNoneNoneNot mentioned
2254
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M12.1 ±0.1Human blood plasma proteasesTLCHuman plasma mixed with drug Clozapinein vitroNoneNoneNot mentioned
2255
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M11.9 ±0.3Human blood plasma proteasesTLCHuman plasma mixed with drug Haloperidolin vitroNoneNoneNot mentioned
2256
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M11.9 ±0.4Human blood plasma proteasesTLCHuman plasma mixed with drug Sulpiridein vitroNoneNoneNot mentioned
2257
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M11.3 ±0.4Human blood plasma proteasesTLCHuman plasma mixed with drug Thiothixenein vitroNoneNoneNot mentioned
2258
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M31.3 ±0.7Human blood plasma proteasesTLCHuman plasma mixed with Bacitracinin vitroNoneNoneNot mentioned
2259
124442982001
YGGFL
Leucine Enkephalin5FreeFreeLinearLNoneHuman brainRegulation of various physiological and behavioral processes2, 4, 6, 10, 30, 60 and 90, 180 minutes10 €“8 M41.1 ±0.9Human blood plasma proteasesTLCHuman plasma mixed with Bacitracinin vitroNoneNoneNot mentioned
2260
3858801979
GG
5-Fluoro-4-(N-succinamoylglycylglycine benzyl ester)-2(1H)-pyrimidone (compound 11)25-Fluoro-4-N-succinamoylBenzyl ester-2(1H)-pyrimidoneLinearLConjugation of peptide C terminal carboxyl group with amino group of 5 FluorocytosineSyntheticAnticandidalNot givenNot mentioned0.3Sample cells proteasesSpectrophotometrySample cellsin vivoNoneNone5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.62,0.62 and 20 µg/mL respectively.
2265
6413241983
HADGVFTSDFSRLLGQLSAKKYLESLI
Peptide histidine isoleucine27FreeFreeLinearLNonePorcine intestineNeurotransmitter1, 2, 3, 4, 5, 10 and 15 min.4.7 pmoles/kg3.1 ±0.5Human plasma proteasesRadioimmunoassayIntravenous administration to human plasmain vivoNoneNonePHI effect on secretion on gastrointestinal hormone and monitor its effect on gastric secretion of pepsin. PHI infused at 4.7pmoles/kg in human and gastric juice were aspirated by suction, gastric secretion was improved to be in case of PIH.
2267
39220131984
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
Calcitonin gene related peptide37FreeFreeLinearLNoneHuman non-thyroidal tissueVasoactive neuropeptideNot given0.32 pmol/kg6.9 ±0.9 (first phase)Human blood plasma proteasesRadioimmunoassayIntravenous injection into humanin vivohttp://physrev.physiology.org/content/94/4/1099NoneCGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion.
2268
39220131984
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
Calcitonin gene related peptide37FreeFreeLinearLNoneHuman non-thyroidal tissueVasoactive neuropeptideNot given2.56 pmol/kg26.4 ±4.7 (first phase)Human blood plasma proteasesRadioimmunoassayIntravenous injection into humanin vivohttp://physrev.physiology.org/content/94/4/1099NoneCGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion.
2269
40344131985
YGGFL
Leucine enkephalin5FreeFreeLinearLNoneHuman brainAnalgesic20 minutes0.9 nM14.7Human serum proteaseHPLCHuman serumin vitroNoneNoneNot reported
2275
40700161985
GGFMTSEKSQTPLVTL
DTγE( Des-Tyr1-γ-Endorphin) (β-endorphin-(2-17))16FreeFreeLinearLNoneCNS and piyuitary gland of HumansNeuropeptide, non-opioid y-type endorphinsNot given3.1-7.1 µg5.5 (elimination phase)Rat blood proteasesRP-HPLCMale wistar Rats (intravenously)in vivoNoneNoneNot reported
2277
61210021982
PLG
PLG peptide3FreeFreeLinearLTritium labeling at ProlineHypothalamus and pineal glandInteract with dopaminergic system and improve patients of parkinson diseaseNot given2 - 2.5 μg20 (t1/2 elimination)Rat plasma proteasesRadioimmunoassaySubcutaneously injected to rat plasmain vivoNoneNoneRadiolabelled peptide was administered in rats and blood plasma was taken and analysed by HPLC. Brain level of radioactivity increased with time.
2278
61272051982
AGCKNFFWKTFTSC
Somatostatin 1414FreeFreeCyclic (C3-C14)LNoneOvine hypothalamusRegulates the endocrine system and affects neurotransmission and cell proliferation30-45 minute10 µg1.7 ±0.2Dog blood proteasesSS Radioimmunoassay assayIntravenous infusion in Dog plasmain vivohttp://www.anaspec.com/products/product.asp?id=574NoneRadiolabelled peptide was administered in rats and blood plasma was taken and analysed by HPLC. Brain level of radioactivity increased with time.
2279
61272051982
SANSNPAMAPRERKAGCKNFFWKTFTSC
Somatostatin 2828FreeFreeCyclic (C17-C28)LNoneOvine hypothalamusRegulates the endocrine system and affects neurotransmission and cell proliferation30-45 minute20 µg2.8 ±0.3Dog blood plasmaSS Radioimmunoassay assayIntravenous infusion in Dog plasmain vivohttp://www.anaspec.com/products/product.asp?id=574NoneWhen 50ng of SS14 was injected there is 85.1% decreasedportal venous blood flow was observed as compared to percentage of basal flow.
2280
61287701982
AGCKNFFWKTFTSC
Somatostatin 1414FreeFreeCyclic (C3-C14)LNoneOvine hypothalamusRegulates the endocrine system and affects neurotransmission and cell proliferation1 hour1.7nmol2.4cat blood proteaseNot mentionedIntravenous infusion to cat plasmain vivohttp://www.anaspec.com/products/product.asp?id=574NoneWhen 100ng of SS28 is injected there is 73% decreased portal venous blood flow as compared to basal blood flow.
2281
61287701982
SANSNPAMAPRERKAGCKNFFWKTFTSC
Somatostatin 2828FreeFreeCyclic (C17-C28)LNoneOvine hypothalamusRegulates the endocrine system and affects neurotransmission and cell proliferation1 hour4.8nmol6.1cat blood proteaseNot mentionedIntravenous infusion to cat plasmain vivohttp://www.anaspec.com/products/product.asp?id=574NoneGastrin exocrine inhibitor assay were performed. 80 % gastric inhibition observed at 7ug/kg of peptide.
2282
62393071984
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial Natriuretic peptide28FreeFreeCyclic (C7-C23)LNoneHuman heartDepressor and natriuretic activity2 hours1nmol30Rat blood proteasesRP-HPLCIntravenous administered to Ratin vivoNoneNoneGastric exocrine inhibitory assay was performed. 80 % inhibition observed at 8ug/kg body weight of peptide
2283
62393071984
SSCFGGRIDRIGAQSGLGCNSFRY
Atriopeptin 324FreeFreeCyclic (C3-C19)LI125 radiolabeledHuman heartDepressor and natriuretic activity2 hours1nmol2.5Rat blood proteasesRP-HPLCIntravenous administered to Ratin vivoNoneNoneTime course depression is seen and Atropeptin 3 shows 2 time more depressor activity as compared to control alpha heart ANP.
2284
62910991982
WMDF
Cholecystokinin-4 (CCK4)4FreeAmidationLinearLNoneDeudenum of pigIntestinal hormoneNot given50 µM13Human plasma proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2285
62910991982
WMDF
Cholecystokinin-4 (CCK4)4FreeAmidationLinearLNoneDeudenum of pigIntestinal hormoneNot given50 µM<1Rat plasma proteaseHPLCRat Plasmain vitroNoneNoneNot reported
2286
62910991982
YMGWMDF
CCK7 (Cholecystokinin-7)7FreeAmidationLinearLNoneDeudenum of pigIntestinal hormoneNot given50 µM2.5Human blood proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2287
62910991982
DYMGWMDF
CCK8 (Cholecystokinin-8)8FreeAmidationLinearLNoneDeudenum of pigIntestinal hormoneNot given50 µM18Human plasma proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2288
62910991982
DYMGWMDF
CCK8 (Cholecystokinin-8)8FreeAmidationLinearLSulphation of Tyrosine residue at position 2Derivative of natural cholecytokininIntestinal hormoneNot given50 µM50Human plasma proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2289
62910991982
DYMGWMDF
CCK8 (Cholecystokinin-8)8FreeAmidationLinearLNoneDeudenum of pigIntestinal hormoneNot given50 µM5Rat plasma proteaseHPLCRat Plasmain vitroNoneNoneNot reported
2290
62910991982
DYMGWMDF
CCK8 (Cholecystokinin-8)8FreeAmidationLinearLSulphation of Tyrosine residue at position 2Derivative of natural cholecytokininIntestinal hormoneNot given50 µM17Rat plasma proteaseHPLCRat Plasmain vitroNoneNoneNot reported
2291
62910991982
RDYWGWLDF
CCK9 (Cholecystokinin-9)9FreeAmidationLinearLSulphation of Tyrosine residue at position 3Derivative of natural cholecytokininIntestinal hormoneNot given50 µM2.7Human plasma proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2292
62910991982
DRDYMGWMDF
CCK10 (Cholecystokinin-10)10FreeAmidationLinearLSulphation of tyrosine residue at position 4Derivative of natural cholecytokininIntestinal hormoneNot given50 µM30Human blood proteasesHPLCHuman plasmain vitroNoneNoneNot reported
2293
62910991982
DRDYMGWMDF
CCK10 (Cholecystokinin-10)10FreeAmidationLinearLSulphation of tyrosine residue at position 4Derivative of natural cholecytokininIntestinal hormoneNot given50 µM45Rat plasma proteaseHPLCRat Plasmain vitroNoneNoneNot reported
2294
63440711983
MKAIFVLKGWWRTS
E.Coli leader peptide of tryptophan operon14FreeFreeLinearLNoneE.coli trp operonRegulatory peptideNot givenNot mentioned03-AprCell-free (S-30) extracts prepared from E. coli strain W3110 trpR tnaA2 AtrpEA2 rnaRadioactivity decay assay (3H) .Leader peptide is radiolabelled and then decay in radioactivity is measured.Not reportedin vitroNoneNoneNot reported
2295
65224421984
YAFGYPS
Dermorphin7FreeFreeLinearLI125 radiolabeledFrog skinOpiod receptor agonist60 minute500 μg/kg1.3Rat blood proteasesRadioimmunoassay and HPLCIntravenous injection into tail of ratsin vivohttp://www.anaspec.com/products/product.asp?id=450NoneNot reported
2296
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.76 μg16.2 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2297
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.85 μg13.3 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2298
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.75 μg12.4 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2299
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.75 μg12.7 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2300
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.90 μg5.6 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2301
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.80 μg9.4 (t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2302
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.80 μg11.6 (mean t1/2 fast)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2304
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.85 μg49.5 (t1/2 slow)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2307
66059721984
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
Ovine corticotropic releasing factor41FreeFreeLinearLNoneParaventricular nucleus (PVN) of the hypothalamusUsed as a diagnostic test in disease affecting the Hypothalamic pituitary axis0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min.90 μg47.9 (t1/2 slow)Human blood plasma proteasesRadioimmunoassay and HPLC analysisIntravenous administration to human plasmain vivohttp://www.anaspec.com/products/product.asp?id=322NoneNot reported
2311
66587061983
ADSGEGDFLAEGGGVR
125I-labeled desamino-tyrosyl (DAT-FPA) FPA16FreeFreeLinearLDAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-TDesaminotyrosine Fibrinopeptide derivativeBlood clotting6 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA7 (radioactivity)Normal rabbit blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of normal rabbitin vivohttp://search.anaspec.com/?keywords=fibrinopeptideNoneNot reported
2312
66587061983
ADSGEGDFLAEGGGVR
125I-labeled desamino-tyrosyl (DAT-FPA) FPA16FreeFreeLinearLDAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-TDesaminotyrosine Fibrinopeptide derivativeBlood clotting7 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA30 (radioactivity)Normal rabbit blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of normal rabbitin vivohttp://search.anaspec.com/?keywords=fibrinopeptideNoneNot reported
2315
66587061983
ADSGEGDFLAEGGGVR
Human Fibrinopeptide A (FPA)16FreeFreeLinearLNoneN terminal end of the A-alpha chain of fibrinogenBlood clotting10 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA3.5Normal rabbit blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of normal rabbitin vivoNoneNoneNot reported
2316
66587061983
ADSGEGDFLAEGGGVR
Human Fibrinopeptide A (FPA)16FreeFreeLinearLNoneN terminal end of the A-alpha chain of fibrinogenBlood clotting11 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA15Normal rabbit blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of normal rabbitin vivoNoneNoneNot reported
2319
66587061983
ADSGEGDFLAEGGGVR
125I-labeled desamino-tyrosyl (DAT-FPA) FPA16FreeFreeLinearLDAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-TDesaminotyrosine Fibrinopeptide derivativeBlood clotting3 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA7 (radioactivity)Nephrectomized rabbits blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of nephrectomized rabbitsin vivoNoneNoneNot reported
2321
66587061983
ADSGEGDFLAEGGGVR
Human Fibrinopeptide A (FPA)16FreeFreeLinearLNoneN terminal end of the A-alpha chain of fibrinogenBlood clotting5 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120 minLabeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA4Nephrectomized rabbits blood proteasesGel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma.Intravenous injection in lateral vein of nephrectomized rabbitsin vivohttp://search.anaspec.com/?keywords=fibrinopeptideNoneNot reported
2322
67362051984
VPLPAGGGTVLTKMYPRGNHWAVGHLM
Gastrin releasing peptide27FreeFreeLinearLNonePorcine nonantral gastric juiceStimulate release of gastrinNot givenGRP I (0-30 min) bolus injection of 1.41 pmol kg-1, followed by an infusion of 0.12 pmol kg-1 x min-2.8 ±0.4 minHuman serum proteasesRadioimmunoassayHuman serumin vivohttp://www.anaspec.com/products/product.asp?id=301NonePlasma gastrin concentration increased immediately after administration of peptide intravenously. After two doses of peptide(1.50pmol/kg) gastrin concentration found to be 1551pmol as compared to basal level of 370pmol.
2324
88396781995
HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Glucagon like peptide 1 (GLP( 7-36))36FreeAmidationLinearLNoneHuman intestinal epitheliumGastric motility5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min400 pmol/l2.1 ±0.1 (for first phase)Dog plasma proteasesRadioimmunoassay and HPLCIntravenous injection to dogs plasmain vitroNoneNoneBacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2325
88396781995
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
Glucagon like peptide 1 (GLP( 7-37))37FreeFreeLinearLNoneHuman intestinal epitheliumGastric motility5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min400 pmol/l2.4 ±0.3 (for first phase)Dog plasma proteasesRadioimmunoassay and HPLCIntravenous injection to dogs plasmain vitrohttp://www.anaspec.com/products/product.asp?id=324NoneBacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased.
2332
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 15, 30, 45, and 60min0.10mg/kg1 (t1/2 α)Rat blood plasma proteasesHPLC-MSIntravenous administered to Ratin vivoNoneNoneNot tested
2333
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min0.10mg/kg13 (t1/2 α)Dog blood plasma proteasesHPLC-MSIntravenous administered to Dogin vivoNoneNoneNot tested
2334
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min0.10mg/kg4 (t1/2 α)Rabbit blood plasma proteasesHPLC-MSIntravenous administered to Rabbitin vivoNoneNoneNot tested
2335
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min0.10mg/kg5 (t1/2 α)Monkey blood plasma proteasesHPLC-MSIntravenous administered to Monkeyin vivoNoneNoneNot tested
2336
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 15, 30, 45, and 60min0.10mg/kg15 (t1/2 β)Rat blood plasma proteasesHPLC-MSIntravenous administered to Ratin vivoNoneNoneNot tested
2341
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min5 mg/kg45 (t1/2 β)Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2342
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min5 mg/kg51Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2347
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day5 mg/kg51Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2353
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day5 mg/kg45Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2354
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day5 mg/kg44Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2355
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day50 mg/kg48Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2356
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day50 mg/kg50Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2359
90626851997
pGlu-NC(C)PRG
[pGIu4,Cyt6]AVP(4-9)6FreeAmidationLinearLpGlu = pyroglutamateHuman kidney cellsAntidiuretic hormone5, 10, 30, 60 and 120 min10 ng/kg40Rat blood proteasesHPLCSubcutaneously injected to ratin vivoNoneNonePassive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2360
90626851997
NCPR
[Cys6]AVP(5-8)4FreeFreeLinearLAt 2 position cystine is replaced by cysteineHuman kidney cellsAntidiuretic hormone5, 10, 30, 60 and 120 min1 ng/kg10Rat blood proteasesHPLCSubcutaneously injected to ratin vivoNoneNonePassive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2361
90626851997
pGlu-NSPRG
No.3026FreeAmidationLinearLpGlu = pyroglutamateHuman kidney cellsAntidiuretic hormone5, 10, 30, 60 and 120 min0.1, 1 and 10ng/kg9Rat blood proteasesHPLCSubcutaneously injected to ratin vivoNoneNonePassive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs.
2363
93570691997
rPKPfQwFwLL
[D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P11FreeAmidationLinearMixNoneSubstance PNeuropeptide growth factor antagonistupto 360 minutes12 µg/g body weight of mice45.9 (terminal t1/2)Mice blood proteasesRP-HPLCIntraperitonial injection to Nu/Nu micein vivohttp://www.abcam.com/d-arg1d-phe5d-trp79leu11-subsNoneNot reported
2366
94214011998
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial Natriuretic peptide28FreeFreeLinearLNoneHuman Heart muscle cellsAntihypertensive0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min2 μg7.7 ±0.8 (t1/2 slow phase)Rat plasma proteasesRadioimmunoassayExogenously administered to Male SHR-SP/Izm rats treated with carvedilolin vivoNoneNoneANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group.
2367
94214011998
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial Natriuretic peptide28FreeFreeLinearLNoneHuman Heart muscle cellsAntihypertensive0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min2 μg4.9 ±0.5 (t1/2 slow phase)Rat plasma proteasesRadioimmunoassayExogenously administered to Male SHR-SP/Izm ratsin vivoNoneNoneANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group.
2371
103544131999
YGG
Thioimreg compound 113FreeFreeLinearLPeptide bonds at position 1,2 was replaced by thioamide linkagesThioanalogue of natural ImregImmunostimulant3.5 hoursNot given46Rat blood proteasesHPLCRat whole bloodin vitroNoneNone125 mg/kg of 11 resulted in a significant increase in activated T helper cells (CD4+CD45+, 28%, P e 0.048). This is accompanied by a significant reduction in NK cells (20-27%, P e 0.02) at 50 and 100 mg/kg
2372
103544131999
YGG
Imreg3FreeFreeLinearLNoneHuman leucocyteImmunostimulant and in clinical trial to treat AIDS3.5 hoursNot given<1Rat blood proteasesHPLCRat whole bloodin vitroNoneNoneImmunophenotyping assay is performed to study immunological effect like stimulation of NK cells and lymphoproliferative properties. T cell proliferation was observed at even at 100mg/kg
2374
105732951999
DPLPEF
Enkephalin6FreeAmidationLinearLNoneNatural (Human brain)Analgesic0, 60, 120, 180, and 300 min1mM30Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2386
107083071999
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive intestinal peptide28FreeFreeLinearLI125 radiolabeling and encapsulation of VIP in LiposomePorcine intestineRelaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min0.33 nM5.29 ±0.62 (t1/2 elimination)Rat plasma proteasesNot mentionedIntravenously administration to rat plasmain vivoPMID 5450698NoneNot tested
2388
107083071999
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive intestinal peptide28FreeFreeLinearLI125 radiolabeling and encapsulation of VIP in LiposomePorcine intestineRelaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min0.33 nM9.28 ±0.76 (t1/2 elimination)Rat lung proteasesNot mentionedIntravenously administration to rat lungin vitroPMID 5450698NoneNot tested
2389
107083071999
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive intestinal peptide28FreeFreeLinearLI125 radiolabelingPorcine intestineRelaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min0.33 nM3.18 ±0.22 (t1/2 elimination)Rat lung proteasesNot mentionedIntravenously administration to rat lungin vitroPMID 5450698NoneNot tested
2390
109738452000
MEPLGWQLTSGPNQEQVSPLTLLK
Alpha 2-antiplasmin (α2AP )24FreeFreeLinearLI125 radiolabelingHuman SERPINF2 geneClotting factor2 hours2 mg/ml19Mouse blood proteasesNot mentionedMouse blood fibrin clotsin vitroNoneNoneImmunoblotting assay was done by taking 50 µL of fibrin clots with 2mg/ml of alpha2 AP and alpha2 AP peptide and cross linking was determined by electroblotting to PVDF membrane and detected by streptavidin-peroxidase.
2391
109738452000
NQEQVSPLTLLK
Alpha 2-antiplasmin peptide (α2AP13-24 )12FreeFreeLinearLBiotinylation at lysine residue(position 24)Human SERPINF2 geneClotting factor2 hours0.5mMol/L21Mouse blood proteasesNot mentionedMouse blood fibrin clotsin vitroNoneNoneImmunoblotting assay was done by taking 50 µL of fibrin clots with 2mg/ml of alpha2 AP and alpha2 AP peptide and cross linking was determined by electroblotting to PVDF membrane and detected by streptavidin-peroxidase.
2392
111455792001
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin like growth factor 1 (IGF-1)70FreeFreeLinearLI125 radiolabelingHuman IGF-1Regulate somatic growth and cellular proliferation1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h15 μCi(0.2 ml)0.033 ±0.004 (t1/2 α)Rat blood proteasesTCA precipitationIntravenous injection into ratin vivoPMID:7758431NoneHuman articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2395
111455792001
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Analogue of Insulin like growth factor 1 (F49A)70FreeFreeLinearLI125 radiolabelingHuman IGF-1Regulate somatic growth and cellular proliferation1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h15 μCi(0.2 ml)0.064 ±0.052 (t1/2 α)Rat blood proteasesTCA precipitationIntravenous injection into ratin vivoPMID:7758431NoneHuman articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2396
111455792001
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Analogue of Insulin like growth factor 1 (F49A)70FreeFreeLinearLI125 radiolabelingHuman IGF-1Regulate somatic growth and cellular proliferation1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h15 μCi(0.2 ml)0.971 ±0.336 (t1/2 β)Rat blood proteasesTCA precipitationIntravenous injection into ratin vivoPMID:7758431NoneHuman articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2398
111455792001
GPATLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Analogue of Insulin like growth factor 1 (E3A/F49A)70FreeFreeLinearLI125 radiolabelingHuman IGF-1Regulate somatic growth and cellular proliferation1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h15 μCi(0.2 ml)0.032 ±0.005 (t1/2 α)Rat blood proteasesTCA precipitationIntravenous injection into ratin vivoPMID:7758431NoneHuman articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2399
111455792001
GPATLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Analogue of Insulin like growth factor 1 (E3A/F49A)70FreeFreeLinearLI125 radiolabelingHuman IGF-1Regulate somatic growth and cellular proliferation1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h15 μCi(0.2 ml)0.321 ±0.0.091 (t1/2 β)Rat blood proteasesTCA precipitationIntravenous injection into ratin vivoPMID:7758431NoneHuman articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter.
2404
45720611972
pGlu-HWSTGLRPG
Luteinizing Hormone Releasing Hormone(LHRH)10FreeAmidationLinearLpGlu=pyroglutamic acid, Tritium labelingGonadotropic cells in the anterior pituitary glandBehavior influencing hormones2 minutes1 .0 μCi6.97 ±0.4Female Sprague Dawley rats blood proteaseRadioimmunoassayIntarvenous administration to Female Sprague Dawley ratsin vivoNoneNoneLH-RH acts on the anterior pituitary to evoke the release of LH
2414
90400911997
pGlu-HWSYwLRP
Meterelin9FreeEthylamideLinearMixpGlu=pyroglutamic acidGonadotropic cells in the anterior pituitary glandBehavior influencing hormones5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an10 μg/kg5.9 ±2.5 (t1/2 α)New Zeland female rabbits blood proteaseRadioimmunoassayIntravenous injected in New Zeland female rabbitsin vivoNoneNoneCastrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2416
90400911997
pGlu-HWSYwLRP
Meterelin9FreeEthylamideLinearMixpGlu=pyroglutamic acidGonadotropic cells in the anterior pituitary glandBehavior influencing hormones5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an1 μg/kg6.6 ±2.7 (t1/2 α)New Zeland female rabbits blood proteaseRadioimmunoassaySubcutaneous injected in New Zeland female rabbitsin vivoNoneNoneCastrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2418
90400911997
pGlu-HWSYwLRP
Meterelin9FreeEthylamideLinearMixpGlu=pyroglutamic acidGonadotropic cells in the anterior pituitary glandBehavior influencing hormones5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an10 μg/kg5.3 ±1.1 (t1/2 α)New Zeland female rabbits blood proteaseRadioimmunoassaySubcutaneous injected in New Zeland female rabbitsin vivoNoneNoneCastrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2420
90400911997
pGlu-HWSYwLRP
Meterelin9FreeEthylamideLinearMixpGlu=pyroglutamic acidGonadotropic cells in the anterior pituitary glandBehavior influencing hormones5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an100 μg/kg7.8 ±2.0 (t1/2 α)New Zeland female rabbits blood proteaseRadioimmunoassaySubcutaneous injected in New Zeland female rabbitsin vivoNoneNoneCastrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days
2424
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng8Rat Stomach luminal flushing proteasesTCA precipitationRat Stomach luminal flushingin vitro632300NoneStimulate gut growth and repair
2425
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng5Rat Stomach luminal flushing proteasesAntibody assayRat Stomach luminal flushingin vitro632300NoneStimulate gut growth and repair
2426
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng2.5Rat Stomach luminal flushing proteasesReceptor-precipitable radioactivityRat Stomach luminal flushingin vitro632300NoneStimulate gut growth and repair
2427
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Duodenum luminal flushing proteasesTCA precipitationRat Duodenum luminal flushingin vitro632300NoneStimulate gut growth and repair
2428
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Duodenum luminal flushing proteasesAntibody assayRat Duodenum luminal flushingin vitro632300NoneStimulate gut growth and repair
2429
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Duodenum luminal flushing proteasesReceptor-precipitable radioactivityRat Duodenum luminal flushingin vitro632300NoneStimulate gut growth and repair
2430
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Ileum luminal flushing proteasesTCA precipitationRat Ileum luminal flushingin vitro632300NoneStimulate gut growth and repair
2431
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Ileum luminal flushing proteasesAntibody assayRat Ileum luminal flushingin vitro632300NoneStimulate gut growth and repair
2432
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Ileum luminal flushing proteasesReceptor-precipitable radioactivityRat Ileum luminal flushingin vitro632300NoneStimulate gut growth and repair
2433
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng38Rat Colon luminal flushing proteasesTCA precipitationRat Colon luminal flushingin vitro632300NoneStimulate gut growth and repair
2434
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng33Rat Colon luminal flushing proteasesAntibody assayRat Colon luminal flushingin vitro632300NoneStimulate gut growth and repair
2435
75616321995
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Growth Hormone5, 10, 20, 30 or 60 min8.6ng16Rat Colon luminal flushing proteasesReceptor-precipitable radioactivityRat Colon luminal flushingin vitro632300NoneStimulate gut growth and repair
2436
75616321995
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)8313 amino acid extension peptide at the N-terminus of IGF-IFreeLinearLI125 labelingAnalogue of IGF-IGrowth Hormone5, 10, 20, 30 or 60 min8.6ng50Rat Stomach luminal flushing proteasesTCA precipitationRat Stomach luminal flushingin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneProtect the growth factor by steric hindrance of cleavage sites.
2437
75616321995
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)8313 amino acid extension peptide at the N-terminus of IGF-IFreeLinearLI125 labelingAnalogue of IGF-IGrowth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Duodenum luminal flushing proteasesTCA precipitationRat Duodenum luminal flushingin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneProtect the growth factor by steric hindrance of cleavage sites.
2438
75616321995
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)8313 amino acid extension peptide at the N-terminus of IGF-IFreeLinearLI125 labelingAnalogue of IGF-IGrowth Hormone2-5, 5, 7-5, 10 or 20min8.6ng2Rat Ileum luminal flushing proteasesTCA precipitationRat Ileum luminal flushingin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneProtect the growth factor by steric hindrance of cleavage sites.
2439
75616321995
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)8313 amino acid extension peptide at the N-terminus of IGF-IFreeLinearLI125 labelingAnalogue of IGF-IGrowth Hormone5, 10, 20, 30 or 60 min8.6ng60Rat Colon luminal flushing proteasesTCA precipitationRat Colon luminal flushingin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneProtect the growth factor by steric hindrance of cleavage sites.
2451
75291081994
CSCSSLMDKECVYFCHLDIIW
Human endothelin-1 (Human ET-1)21FreeFreeLinearLNoneHuman Endothelin-1Vasoconstricting peptide180 minute3 nmol of peptide with 200 ng of enzyme37 (t1/2 of hydrolysis)Endopeptidase-24.11(E-24.11)Radioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitro8269939NoneNot reported
2452
75291081994
VNTPEHVVPYGLGSPRS
C-terminal fragment of Human Endothelin-1 (CTF)17FreeFreeLinearLNoneHuman Endothelin-1Vasoconstricting peptide180 minute3 nmol of peptide with 200 ng of enzyme57 (t1/2 of hydrolysis)Endopeptidase-24.11(E-24.11)Radioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitro8269939NoneNot reported
2453
75291081994
CSCSSLMDKECVYFCHLDIIWVNTPERVVPYGLGSPSRS
Porcine big endothelin-1 (Porcine big-ET-1)39FreeFreeLinearLNonePorcine Endothelin-1Vasoconstricting peptide80 minute3 nmol of peptide with 50 ng of enzyme25 (t1/2 of hydrolysis)ThermolysinRadioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitro8269939NoneNot reported
2454
75291081994
CSCSSLMDKECVYFCHLDIIW
Porcine endothelin-1 (Porcine ET-1)21FreeFreeLinearLNonePorcine Endothelin-1Vasoconstricting peptide80 minute3 nmol of peptide with 50 ng of enzyme56 (t1/2 of hydrolysis)ThermolysinRadioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitro8269939NoneNot reported
2455
75291081994
VNTPERVVPYGLGSPSRS
C-terminal fragment of Porcine Endothelin-1 (Porcine CTF)18FreeFreeLinearLNonePorcine Endothelin-1Vasoconstricting peptide80 minute3 nmol of peptide with 50 ng of enzyme47 (t1/2 of hydrolysis)ThermolysinRadioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitro8269939NoneNot reported
2456
75291081994
RPKPQQFFGLM
Substance P11FreeFreeLinearLNoneSpinal cordVasoconstricting peptide180 minute3 nmol of peptide with 200 ng of enzyme2.1 (t1/2 of hydrolysis)Endopeptidase-24.11(E-24.11)Radioimmunoassay and RP-HPLCPurified ET-1 protein samplein vitroNoneNoneNot reported
2457
76894991993
GWTLNSAGYLLGPHAVGNHRSFSDKNGLTS
Galanin30FreeFreeLinearLNoneHuman tissueNeuropeptide60 minutes74 pmol/kg3.7 ±0.4Human serum proteasesRadioimmunoassayHuman serumin vivo1370155NoneGrowth hormone concentrations increased markedly during galanin infusion reaching a plateau value eight times the pre-infusion concentrations after 40-min infusion p < 0.01
2458
77147461994
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneOpoidNociception regulating peptideNot mentioned0.10mM, 10 mL17.7Aminopeptidases present in nasal mucosa of ratHPLCNasal administration to Male Sprague Dawley derived ratsin vivoNoneNoneNot reported
2459
77147461994
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneOpoidNociception regulating peptideNot mentioned0.10mM, 10 mL23.9Aminopeptidases present in nasal mucosa of ratHPLCNasal administration to Male Sprague Dawley derived ratsin vivoNoneNoneNot reported
2460
77147461994
DGGFL
Leu-enkephalin analogue5FreeFreeLinearLNoneOpoidNociception regulating peptideNot mentioned0.10mM, 10 mL21.2Aminopeptidases present in nasal mucosa of ratHPLCNasal administration to Male Sprague Dawley derived ratsin vivoNoneNoneNot reported
2461
79575361994
HwAWfK
Hexarelin6FreeAmidationLinearMixTrp methylated at position 2Growth hormone-releasing hormone-6Growth hormone-releasing peptide24 hours0.5 μg/kg50Human serum proteasesChemiluminescence immunometric assayTwelve adult male volunteersin vivoNoneNoneMean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg
2462
79575361994
HwAWfK
Hexarelin6FreeAmidationLinearMixTrp methylated at position 2Growth hormone-releasing hormone-6Growth hormone-releasing peptide24 hours1 μg/kg51Human serum proteasesChemiluminescence immunometric assayTwelve adult male volunteersin vivoNoneNoneMean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg
2463
79575361994
HwAWfK
Hexarelin6FreeAmidationLinearMixTrp methylated at position 2Growth hormone-releasing hormone-6Growth hormone-releasing peptide24 hours2 μg/kg58Human serum proteasesChemiluminescence immunometric assayTwelve adult male volunteersin vivoNoneNoneMean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg
2464
79914431994
YEPGKSSILQHERPVTKPQA
C-20 Sorbin20FreeAmidationLinearLNoneDerived from SorbinElectrolyte absorbing peptide1, 2, 4, 8, 16, and 32 min200 μg/kg/h9.5 ±1.8Rat blood proteasesRadioimmunoassayMale Sprague-Dawley rats bloodin vivoNoneNoneIncreases absorption of water and ions
2465
79914431994
YEPGKSS
C-7 Sorbin7FreeAmidationLinearLNoneDerived from SorbinElectrolyte absorbing peptide1, 2, 4, 8, 16, and 32 min200 μg/kg/h7.5 ±1.5Rat blood proteasesRadioimmunoassayMale Sprague-Dawley rats bloodin vivoNoneNoneIncreases absorption of water and ions
2466
79914431994
YEPGKSS
Tritiated C-7 Sorbin7FreeAmidationLinearL[2-dehydro-Pro1.5]C is attached and tritiatedDerived from SorbinElectrolyte absorbing peptide1, 2, 4, 8, 16, 32, and 64 min2.8 MBq17.9 ±1.5Rat blood proteasesRadioimmunoassayMale Sprague-Dawley rats bloodin vivoNoneNoneIncreases absorption of water and ions
2469
80769091994
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Human BNP (Brain natriuretic Peptide)32FreeFreeLinearLNoneHuman BNP (Brain Natriuretic Peptide)Diuretic,natriuretic and vasodilatory peptideNot mentionedNot mentioned20.7 (slow component)NoneNot mentionedNonein vitro2136732NoneNot reported
2470
80769091994
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
Human BNP (Brain natriuretic Peptide)32FreeFreeLinearLNoneHuman BNP (Brain Natriuretic Peptide)Diuretic,natriuretic and vasodilatory peptideNot mentionedNot mentioned3.9 (fast component)NoneNot mentionedNonein vitro2136732NoneNot reported
2471
80769091994
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Human BNP (Brain natriuretic Peptide)28FreeFreeLinearLNoneHuman BNP (Brain Natriuretic Peptide)Diuretic,natriuretic and vasodilatory peptideNot mentionedNot mentioned13.3 (slow component)NoneNot mentionedNonein vitro6223192NoneNot reported
2472
80769091994
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Human BNP (Brain natriuretic Peptide)28FreeFreeLinearLNoneHuman BNP (Brain Natriuretic Peptide)Diuretic,natriuretic and vasodilatory peptideNot mentionedNot mentioned1.7 (fast component)NoneNot mentionedNonein vitro6223192NoneNot reported
2473
80827051994
EAKSQGGSN
Facteur thymique serique9FreeFreeLinearLNoneThymic peptide hormoneThymic hormone used to treat autoimmune disorder5 minutes300-500 kBq/kg02-MarRats blood proteasesRadioimmunoassayIntravenouly injected in male Wistar ratsin vivo7011613NoneThe basal IRI level at 24 h after alloxan injection was significantly lower in alloxan-treated samples than in controls (12.1 + 5.2 vs. 28.7 + 6.3/zU/ml, P < 0.05)
2474
81940821993
NSDSECPLSHDGYCLHDGVCMYIEALDKYACNCVVGYIGERCQYRDLKWWELR
Epidermal Growth Factor (EGF)53FreeFreeLinearLI125 labelingEpidermal Growth FactorGrowth factor135 minutes1420 Ci/mmol12.4 (dissociation t1/2)Proteases present in human meningiomaAutoradiographyFresh surgically excised human meningioma specimensin vitro4636327NoneHigh concentrations (10-4-10 -2 M) of suramin inhibited 125I-EGF binding to meningioma sections with ICs0's of 3.2 + 0.4 × 1 0 - 4 M
2477
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Adrenomedullin (AM)50FreeAmidationLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes1.0 nmol/kg, dissolved in saline1.05 ±0.04Rat blood proteasesRadioimmunoassaySpontaneously hypertensive rats (SHR)in vivoNoneNoneThe mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg.
2478
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Adrenomedullin (AM)51FreeAmidationLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes1.0 nmol/kg, dissolved in saline1.19 ±0.09Rat blood proteasesRadioimmunoassayWistar-Kyoto ratsin vivoNoneNoneThe mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg.
2479
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Adrenomedullin (AM)52FreeAmidationLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes1.0 nmol/kg, dissolved in saline18.1 ±1.4Rat blood proteasesRadioimmunoassaySpontaneously hypertensive rats (SHR)in vivoNoneNoneThe mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg.
2480
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Adrenomedullin (AM)53FreeAmidationLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes1.0 nmol/kg, dissolved in saline16.3 ±1.2Rat blood proteasesRadioimmunoassayWistar-Kyoto ratsin vivoNoneNoneThe mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg.
2481
85452411995
YGGFLRRIRPKLKWDN
Dynorphin A (DYN A) analog-117FreeFreeLinearLNoneOpoidPhysiological effect regulating peptide0-60 minutes100 μM peptide solution to 0.18-ml portions of brain membranes42Endopeptidase 24-11 (enkephalinase), mouse brain proteasesHPLCMouse brain homogenatesin vitroNoneNoneNot reported
2483
85452411995
YGGFLRRIRPKLKWDN
Dynorphin A (DYN A) analog-317FreeFreeLinearLThe reduced bond psi [CH,-NH] was introduced at position 3-4OpoidPhysiological effect regulating peptide0-60 minutes100 μM peptide solution to 0.18-ml portions of brain membranes43Endopeptidase 24-11 (enkephalinase), mouse brain proteasesHPLCMouse brain homogenatesin vitroNoneNoneNot reported
2491
85452551995
HwAWfK
Hexarelin6FreeFreeLinearMixMethylated at position 2 of D-trpGrowth hormone-releasing hormone-6Growth hormone-releasing peptide1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.1 μg/kg25 ±5.02Dog blood proteasesRadioimmunoassaySubcutaneous injection to male and female dogsin vivoNoneNoneNot reported
2492
85452551995
HwAWfK
Hexarelin6FreeFreeLinearMixMethylated at position 2 of D-trpGrowth hormone-releasing hormone-6Growth hormone-releasing peptide1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.10 μg/kg33.3 ±8.83Dog blood proteasesRadioimmunoassaySubcutaneous injection to male and female dogsin vivoNoneNoneNot reported
2493
85452551995
HwAWfK
Hexarelin6FreeFreeLinearMixMethylated at position 2 of D-trpGrowth hormone-releasing hormone-6Growth hormone-releasing peptide1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose.100 μg/kg36.7 ±12.01Dog blood proteasesRadioimmunoassaySubcutaneous injection to male and female dogsin vivoNoneNoneNot reported
2495
92343361993
HSDAVFTDNYTRLRKQMAVKKYLNSILN
Vasoactive intestinal peptide (VIP)28FreeFreeLinearLNoneSmall intestinal mucosaVasoactive peptide2,3,6,10,20,40,60 minutes250 μg2.3 ±0.8Rat blood proteasesRadioimmunoassayIntravenous injection to Rat bloodin vivohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneRegulate of blood flow and smooth muscle relaxation in specific mammalian organs
2507
128527702003
pGlu-LYENKPRRPYIL
Neurotensin13FreeFreeLinearLPost translationaly modified Glu residue at first positionBovine hypothalamusNeuromodulator peptide24 hour50 μg/well1.5Mice blood proteasesHPLCNTR-positive HT29 tumor- bearing SCID micein vivoNoneNoneIC50 value reported was 0.2 nM
2511
157404582005
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat AM (Adrenomedullin)50FreeFreeLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes200 μl2 (distribution t1/2)Rat blood proteasesCompetitive RadioimmunoassayIntravenous administration in Ratin vivohttp://www.anaspec.com/products/product.asp?id=304NoneNot reported
2512
157404582005
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat AM (Adrenomedullin)50FreeFreeLinearLNoneHuman pheochromocytomaHypotensive peptide30 minutes200 μl15.9 (elimination t1/2)Rat blood proteasesCompetitive RadioimmunoassayIntravenous administration in Ratin vivohttp://www.anaspec.com/products/product.asp?id=304NoneNot reported
2513
163022712006
GKAFRR
Human Glandular Kallikrein 2 (hK2)-activated thapsigargin prodrug6AcetylationFreeLinearLLigated with potent cytotoxin thapsigargin, L12ADTHuman glandular kallikrein 2 (hK2)Antitumor peptide24 hours6 mg/kg40Mice blood proteasesNot mentionedBalb-C micein vivoNoneNoneIntratumoral concentrations reached levels comparable to the in vitro IC50 of the prodrug with concentrations of 1.25 mM seen at 1 and 4 hr.
2514
170653942006
AKPEAPGEDASPEELSRYYASLRHYLNLVTRQRY
Porcine PYY (Peptide YY)34FreeAmidationLinearLNonePorcine intestineNeuropeptide120 minutes25 mg/kg BW per min15Pigs blood proteasesDouble-antibody RadioimmunoassayIntravenously administred to Crossbred (Large White!Landrace!Duroc) castrated male pigsin vivohttp://www.genscript.com/peptide/RP10354-Peptide_YNonePlasma GH levels significantly increased 30 min after PYY3 €“36 injection compared with the saline-injected group (7.8 ± 2.1 vs 3.0 ± 0.6 ng/ml, P<0.05)
2515
175839272007
RXRRXRRXRRXRXB
Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO)34FreePMO (5'-ACGTTGAIIIGCATCGTCGC-3')LinearLX = 6-aminohexanoic acid, B = beta-alanine, I = inosineCell penetrating peptides-Phosphorodiamidate morpholino oligomersCell penetrating peptide24 hours15 mg/kg0.40 ±0.05 (t1/2 α)Rat plasma proteasesMALDI-TOF-MSIntravenous administration in Ratin vitroNoneNoneLD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg
2516
175839272007
RXRRXRRXRRXRXB
Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO)34FreePMO (5'-ACGTTGAIIIGCATCGTCGC-3')LinearLX = 6-aminohexanoic acid, B = beta-alanine, I = inosineCell penetrating peptides-Phosphorodiamidate morpholino oligomersCell penetrating peptide24 hours30 mg/kg0.63 ±0.02 (t1/2 α)Rat plasma proteasesMALDI-TOF-MSIntravenous administration in Ratin vitroNoneNoneLD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg
2524
83884031993
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic Peptide)28FreeFreeLinearLNoneHuman HeartDiuretic,natriuretic and vasodilatory peptide2 hours1.5 pmol/lg/min4.1 ±0.4Human serum proteasesRadioimmunoassayHuman serumin vivohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo significant differences in systolic blood pressure, diastolic blood pressure or pulse rate were observed when values on active and placebo infusions were compared (P = 0.85)
2526
38716101985
PSSSLHLHRRITHHRRLGCFRSSGSLLNNAMKGGVDDEITLSAYITMALLESSLPDTDP
Rat α1- proteinase inhibitor60FreeFreeLinearLNoneRat serumProtelytic activities regulating peptide5 minutes, 30 minutes, 1 hour, 4 hour and 7 hourNot mentioned30 (for unglycosylated α1- proteinase inhibitor)Rat serum proteasesRadioimmunoassayWistar ratsin vivohttp://www.uniprot.org/uniprot/Q9JMK6NoneProtect tissue against proteolytic attack by leukocyte elastase
2527
64330081984
pGlu-HYSTlLAP-des-Gly
TAP-14410FreeEthylamideLinearMixpGlu=pyroglutamic acid, des-GlyLHRH derivativeGonadotrophins secreting hormone10 days10μg/100g body wt32 (t1/2 terminal phase)Rat serum proteasesNot mentionedSubcutaneous administration to Sprague-Dawley ratsin vivoNoneNoneSerum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration
2530
64330081984
pGlu-HYSTlLAP-des-Gly
TAP-14410FreeEthylamideLinearMixpGlu=pyroglutamic acid, des-GlyLHRH derivativeGonadotrophins secreting hormone10 days100μg/100g body wt55.5 (t1/2 terminal phase)Rat serum proteasesNot mentionedRectal administration to Sprague-Dawley ratsin vivoNoneNoneSerum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration
2531
64330081984
pGlu-HYSTlLAP-des-Gly
TAP-14410FreeEthylamideLinearMixpGlu=pyroglutamic acid, des-GlyLHRH derivativeGonadotrophins secreting hormone10 days100μg/100g body wt43.7 (t1/2 terminal phase)Rat serum proteasesNot mentionedNasal administration to Sprague-Dawley ratsin vivoNoneNoneSerum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration
2533
106079402000
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow5, 30, 120 and 240 min100 μl3.2 ±0.1 (t1/2α)Rat blood proteasesRadioimmunoassay and bi-exponential equation that describes a two-compartment modelIntravenous bolus administration in Ratin vivo632300Noneinfusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid.
2534
106079402000
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Insulin-like growth factor-I (IGF-I)70FreeFreeLinearLI125 labelingHuman IGF-1Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow5, 30, 120 and 240 min100 μl4.9 ±0.02 (t1/2α)Rat blood proteasesRadioimmunoassay and bi-exponential equation that describes a two-compartment modelIntravenous bolus administration in Ratin vivo632300Noneinfusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid.
2535
106079402000
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)83FreeFreeLinearLI125 labelingAnalogue of IGF-IPromotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow5, 30, 120 and 240 min100 μl2.8 ±0.1 (t1/2α)Rat blood proteasesRadioimmunoassay and bi-exponential equation that describes a two-compartment modelIntravenous bolus administration in Ratin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneAt 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid.
2536
106079402000
MFPAMPLSSLFVNGPRTLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
LR(3) insulin-like growth factor-I (IGF-I)83FreeFreeLinearLI125 labelingAnalogue of IGF-IPromotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow5, 30, 120 and 240 min100 μl4.6 ±0.5 (t1/2α)Rat blood proteasesRadioimmunoassay and bi-exponential equation that describes a two-compartment modelIntravenous bolus administration in Ratin vivohttp://www.cellsciences.com/content/p-detail.asp?rNoneAt 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid.
2541
43277301971
SYSMEHFRWGKPVGKKRRPVKVYPAGEDDEASEAFPLEF
Purified Sheep Adrenocorticotropic Hormone (ACTH)39FreeFreeLinearLNoneSheep Adrenocorticotropic Hormone (ACTH)Steroidogenic peptides1/2, 1, 2, 4, 8, and 16min2U7.32 (steriodigenic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivohttp://www.genscript.com/peptide/RP11304-ACTH_1-39NoneShows activity of 80~180USP Units/mg
2542
43277301971
GYSMEHFRYGKPVGKKRR
ACTH analogue- 318FreeAmidationLinearLNoneOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16min5 μg2.6 (steriodigenic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneNo odification in the activity of ACTH analog-2 peptide
2543
43277301971
βAla-YSMEHFRYGKPVGKKRR
ACTH analogue- 418FreeAmidationLinearLβAla = Beta alanineOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned7.32 (steriodigenic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShowed higher potencies than Native ACTH in all the method tested
2544
43277301971
Ibu-YSMEHFRYGKPVGKKRR
ACTH analogue- 518FreeAmidationLinearLIbu = α-aminoisobutyric acidOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned9.6 (steriodigenic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneThe intravenous and intramuscular potencies of peptide V, Ibu1 ACTH (1-18) amide were 480-757U/mg, 4-5 times higher than the values for native hormone but subcutaneous potency was rather low (264U/mg) and in vitro potency was much lower (83U/mg) than the intravenous and intramuscular potencies.
2545
43277301971
βAla-YSMEHFRYGKPVGKKR-Orn
ACTH analogue- 618FreeAmidationLinearLβAla = Beta alanine, Orn = OrnithineOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned10.06 (steriodigenic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShowed an activity about 2/3 of that of the original Lys15 peptides IV
2546
43277301971
SYSMEHFRWGKPVGKKRRPVKVYPAGEDDEASEAFPLEF
Purified Sheep Adrenocorticotropic Hormone (ACTH)39FreeFreeLinearLNoneSheep Adrenocorticotropic Hormone (ACTH)Steroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned4.43 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivohttp://www.genscript.com/peptide/RP11304-ACTH_1-39NoneShows activity of 80~180USP Units/mg
2547
43277301971
GYSMEHFRYGKPVGKKRR
ACTH analogue- 318FreeAmidationLinearLNoneOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned1.95 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShows activity less than ACTH
2548
43277301971
βAla-YSMEHFRYGKPVGKKRR
ACTH analogue- 418FreeAmidationLinearLβAla = Beta alanineOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned3.08 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShows activity less than ACTH
2549
43277301971
Ibu-YSMEHFRYGKPVGKKRR
ACTH analogue- 518FreeAmidationLinearLIbu = α-aminoisobutyric acidOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned3.32 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShows activity less than ACTH
2550
43277301971
βAla-YSMEHFRYGKPVGKKR-Orn
ACTH analogue- 618FreeAmidationLinearLβAla = Beta alanine, Orn = OrnithineOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned4.53 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShows activity less than ACTH
2551
43277301971
Ibu-YSMEHFRYGKPVGKKR-Orn
ACTH analogue- 718FreeAmidationLinearLIbu = α-aminoisobutyric acidOctadecapeptide analogues of ACTHSteroidogenic peptides1/2, 1, 2, 4, 8, and 16minNot mentioned6 (lipolytic activity t1/2)Rat blood proteasesNot mentionedIntravenously injected to ratin vivo4286483NoneShows activity more than ACTH
2552
43277301971
SYSMEHFRWGKPVGKKRRPVKVYPAGEDDEASEAFPLEF
Purified Sheep Adrenocorticotropic Hormone (ACTH)39FreeFreeLinearLNoneSheep Adrenocorticotropic Hormone (ACTH)Steroidogenic peptides1,2,3 and 4 hours200 mU59.22 (lipolytic activity t1/2)Rat plasma proteasesNot mentionedRat plasmain vitrohttp://www.genscript.com/peptide/RP11304-ACTH_1-39NoneNot mentionedtive ACTH shows similar activity to rat and rabbit fats when compared in terms of the minimal effective dose (rat = 6*10-6mg/50mg tissue and rabbit = 5*10-6mg/50mg tissue)
2553
43277301971
GYSMEHFRYGKPVGKKRR
ACTH analogue- 318FreeAmidationLinearLNoneOctadecapeptide analogues of ACTHSteroidogenic peptides1,2,3 and 4 hoursNot mentioned30 (lipolytic activity t1/2)Rat plasma proteasesNot mentionedRat plasmain vitro4286483NoneShowed much higher activity in rabbit fat than in rat fat (rat = 6*10-6mg/50mg tissue and rabbit = 0.4*10-6mg/50mg tissue)
2554
43277301971
βAla-YSMEHFRYGKPVGKKRR
ACTH analogue- 418FreeAmidationLinearLβAla = Beta alanineOctadecapeptide analogues of ACTHSteroidogenic peptides1,2,3 and 4 hours20 μg35.4 (lipolytic activity t1/2)Rat plasma proteasesNot mentionedRat plasmain vitro4286483NoneShowed much higher activity in rabbit fat than in rat fat (rat = 0.6*10-6mg/50mg tissue and rabbit = 0.07*10-6mg/50mg tissue)
2555
43277301971
Ibu-YSMEHFRYGKPVGKKRR
ACTH analogue- 518FreeAmidationLinearLIbu = α-aminoisobutyric acidOctadecapeptide analogues of ACTHSteroidogenic peptides1,2,3 and 4 hours20 μg32.43 (lipolytic activity t1/2)Rat plasma proteasesNot mentionedRat plasmain vitro4286483NoneShowed much higher activity in rabbit fat than in rat fat (rat = 0.2*10-6mg/50mg tissue and rabbit = 0.002*10-6mg/50mg tissue)
2560
43277301971
GYSMEHFRYGKPVGKKRR
ACTH analogue- 318FreeAmidationLinearLNoneOctadecapeptide analogues of ACTHSteroidogenic peptides1,2,3 and 4 hoursNot mentioned42.6 (lipolytic activity t1/2)Rat muscle proteasesNot mentionedRat muscle slicesin vitro4286483NoneShowed much higher activity in rabbit fat than in rat fat (rat = 6*10-6mg/50mg tissue and rabbit = 0.4*10-6mg/50mg tissue)
2567
172832372007
HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
Glucagon like peptide-1 (GLP-1)37FreeFreeLinearLNoneHuman GLP-1Growth Hormone3 hours100 μg/kg peptide in mice<5Mice blood proteasesRadioimmunoassaySubcutaneously injected in micein vivohttp://www.uniprot.org/blast/?about=P01275[92-128]NonePromotes glucose-depen- dent insulin secretion from the pancreas
2570
82184821993
YRGDS
RGD containing peptide5FreeFreeLinearLI125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymerExtra Cellular Matrix proteinsAntitumor peptideNot mentioned0.2 mL0.5 (t1/2 first phase)Mice blood proteasesRadioimmunoassayIntravenously injected to C57BL6 micein vivoNoneNoneLess effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2573
172588192007
CYFQNCPRG
Vasopressin, 8-L-Arginine9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min15 μCi (555 kBq)1.06 ±0.19 (fast phase)Rat blood proteasesRadioimmunoassayFemale homozygous Brattleboro rats and male Wistar ratsin vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantidiuretic activity 408 IU/mg
2574
172588192007
CYFQNCPRG
Vasopressin, 8-L-Arginine9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min15 μCi (555 kBq)5.96 ±0.58 (slow phase)Rat blood proteasesRadioimmunoassayFemale homozygous Brattleboro rats and male Wistar ratsin vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantidiuretic activity 408 IU/mg
2575
172588192007
CYFQNCPRG
Vasopressin, 8-L-Arginine9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min15 μCi (555 kBq)1.00 ±0.15 (fast phase)Rat blood proteasesRadioimmunoassayFemale homozygous Brattleboro rats and male Wistar rats along with OPC-31260in vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantidiuretic activity 408 IU/mg
2576
172588192007
CYFQNCPRG
Vasopressin, 8-L-Arginine9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min15 μCi (555 kBq)8.90 ±0.37 (slow phase)Rat blood proteasesRadioimmunoassayFemale homozygous Brattleboro rats and male Wistar rats along with OPC-31261in vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantidiuretic activity 408 IU/mg
2577
176841032007
CYFQNCPRG
125I-vasopressin9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide1,2 and 3 minutes50 or 0.4 pmol of vasopressin with 33 kBq~ 1.5Mice blood proteasesRadioimmunoassaySaline treated IRAP+/+ micein vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantiduretic activity
2578
176841032007
CYFQNCPRG
125I-vasopressin9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide1,2 and 3 minutes50 or 0.4 pmol of vasopressin with 33 kBq1Mice blood proteasesRadioimmunoassayInsulin-treated IRAP+/+ micein vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantiduretic activity
2579
176841032007
CYFQNCPRG
125I-vasopressin9FreeFreeCyclic (C1-C6)LI125 labelingHuman VasopressinAnti-diuretic peptide1,2 and 3 minutes50 or 0.4 pmol of vasopressin with 33 kBq3Mice blood proteasesRadioimmunoassayInsulin-treated IRAP-/- mice.in vivohttp://www.polypeptide.com/vasopressin-8-l-argininNoneantiduretic activity
2580
158288222005
GViTRIR
Peptide17AcetylationN-EthylmaleimidationLinearMixNoneSecond type 1 repeat of thrombospondin-1Antiangiogenic activityNot mentioned5mg/kg<1Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = >100nM
2581
158288222005
Sar-GViTXIRP
Compond 5 (ABT-526)9AcetylationN-EthylmaleimidationLinearMixSar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.2Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2583
158288222005
Sar-GViTXIRP
Compond 5 (ABT-526)9AcetylationN-EthylmaleimidationLinearMixSar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.5Monkey plasma proteasesNot mentionedMonkey plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2584
158288222005
Sar-GViTXIRP
Compond 5 (ABT-526)9AcetylationN-EthylmaleimidationLinearMixSar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.5Proteases from dog plasmaNot mentionedDog plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM
2585
158288222005
Sar-GViT-(Dallo-Ile)-IRP
Compond 6 (ABT-510)9AcetylationN-EthylmaleimidationLinearMix4th AA is D isoform of allo- Ile, Sar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.2Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2586
158288222005
Sar-GViT-(Dallo-Ile)-IRP
Compond 6 (ABT-510)9AcetylationN-EthylmaleimidationLinearMix4th AA is D isoform of allo- Ile, Sar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.15Mouse plasma proteasesNot mentionedMouse plamsain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2588
158288222005
Sar-GViT-(Dallo-Ile)-IRP
Compond 6 (ABT-510)9AcetylationN-EthylmaleimidationLinearMix4th AA is D isoform of allo- Ile, Sar- SarcosineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.8Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM
2589
158288222005
GViT-(Nva)-IRP
Compund 48AcetylationN-EthylmaleimidationLinearMixSar- Sarcosine, Nva-NorvalineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.3Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 = 0.07 ± 0.004 nM,
2590
158288222005
Sar-GViT-(Nva)-IRP
Compound 79NHIspN-EthylmaleimidationLinearMixSar- Sarcosine , Nva-NorvalineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.9Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 =29 ± 0.003 nM, Inhibition of HMVEC tube formation with IC50 = >1000nM
2591
158288222005
Sar-GViT-(Nva)-IRP
Compound 89SuccinylationN-EthylmaleimidationLinearMixSar- Sarcosine ,Nva-norvalineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.2Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 =0.26 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10-5nM
2592
158288222005
Sar-GViT-(NMeNva)-IRP
Compound 99AcetylationN-EthylmaleimidationLinearMixSar- Sarcosine , NMeNva- N-methyl-norvalineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg1Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 =0.54 ± 0.150 nM, Inhibition of HMVEC tube formation with IC50 = 50-25nM
2594
158288222005
Sar-GViT-NMeNva-IRP
Compound 119SuccinylationN-EthylmaleimidationLinearMixSar- Sarcosine , NMeNva- N-methyl-norvalineSynthetic (derived from peptide 1)Antiangiogenic activityNot mentioned5mg/kg0.3Rat plasma proteasesNot mentionedRat plasmain vivoNoneNoneInhibition of HMVEC migration with IC50 =0.06 ± 0.030 nM, Inhibition of HMVEC tube formation with IC50 = 0.25- 0.10nM
2606
174086662007
ARPYSFGL
Cydiastatin 48FreeAmidationLinearLNoneSyntheticNeuropeptides30 °C for 20 minutes1nmol16.5M. sexta larval midgut tissue proteasesRP-HPLCMidgut tissues of M. sextain vitroNoneNoneNot reported
2607
174086662007
ARPYSFGL
Cydiastatin 58FreeAmidationLinearLNoneSyntheticNeuropeptides30 °C for 20 minutes1nmol2.5M. sexta larval midgut lumen proteasesRP-HPLCMidgut Lumen of M. sextain vitroNoneNoneNot reported
2609
174086662007
PPPPPARPYSFGL
Cydiastatin 4-alpha13FreeAmidationLinearLNoneSyntheticNeuropeptides30 °C for 20 minutes1nmol4.5M. sexta larval midgut lumen proteasesRP-HPLCMidgut lumen of M. sextain vitroNoneNoneNot reported
2610
174086662007
PPPPPARPYSFGL
Cydiastatin 4-alpha13FreeAmidationLinearLNoneSyntheticNeuropeptides31 °C for 20 minutes1nmol52M. sexta haemolymph proteasesRP-HPLCHaemolymph of M. sextain vitroNoneNoneNot reported
2612
174086662007
PPPPPARPYSF-(Acpc)
Cydiastatin 4-alpha12FreeAmidationLinearLAcpc=cyclopropylalanineSyntheticNeuropeptides30 °C for 20 minutes1nmol7.5M. sexta larval midgut lumen proteasesRP-HPLCMidgut lumenin vitroNoneNoneNot reported
2613
174989582007
Pyr-HP
Thyrotropin-releasing hormone (TRH)3FreeAmidationLinearLPyr=pyroglutamic acidHypothalamusStimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland37 °C for 1-120 minutes200μM~3Homogenate of Caco-2 cells proteasesLC-MSHomogenate of Caco-2 cellsin vitroNoneNoneNot reported
2614
174989582007
Pyr-HP
Peptide1 (Thyrotropin-releasing hormone (TRH) analogue)3FreeD-glucopyranuronamideLinearLPyr=pyroglutamic acidSynthetic derived from TRHStimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland37 °C for 1-120 minutes200μM~20Homogenate of Caco-2 cells proteasesLC-MSHomogenate of Caco-2 cellsin vitroNoneNoneNot reported
2615
174989582007
QHP
Peptide2 (Thyrotropin-releasing hormone (TRH) analogue)32-aminooctanoic acidD-glucopyranuronamideLinearLNoneSynthetic derived from TRHStimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland37 °C for 1-120 minutes200μM~20Homogenate of Caco-2 cells proteasesLC-MSHomogenate of Caco-2 cellsin vitroNoneNoneNot reported
2616
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide3.2mg/kg8.15 ±1.97 ( alpha or distribution half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2617
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide6.4mg/kg9.69 ±1.5 ( alpha or distribution half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2618
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide12.8mg/kg8.56 ±2.01 ( alpha or distribution half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2619
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide3.2mg/kg24.74 ±8.30 ( beta or elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2620
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide6.4mg/kg27.38 ±11.52 ( beta or elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2621
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide12.8mg/kg30.49 ±10.24 ( beta or elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2622
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide3.2mg/kg1.45 ±0.53(gamma or termination elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2623
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide6.4mg/kg1.30 ±0.27 (gamma or termination elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2624
180493082007
FPESKATNATLDPRPGGGGNGDFEEIPEEYLQ
HLP(Hirulog-like peptide)32FreeFreeLinearLI125 labelingSyntheticThrombin inhibitorBlood collected after 2-120 minutes after i/v injection of peptide12.8mg/kg1.24 ±0.44 (gamma or termination elimination half life)Rat plasma proteasesRadioisotopic tracing methodRat plasmain vivoNoneNonePlatelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control
2626
175320972007
FGGFTGARKSARKLANQ
N/OFQ (Nociceptin/Orphanin FQ peptide receptor)17FreeFreeLinearLNoneDerived from the prepronociceptin proteinNOP-Receptor ligands37 °C for 240 min6 μg/μl3.2 ±1.8Mouse brain homogenate proteasesRP-HPLCMouse brain homogenatein vitroNoneNoneHypotensive and bradycardic effects evoked by N/OFQ after i.v. administration in rats, was lasting (about 10 min)
2627
175320972007
FGG-(pF)F-TG-Aib-RKSARKRKNQ
UFP-112 (Nociceptin/Orphanin FQ receptor antagonist)17FreeAmidationLinearL(pF)F = p-flouro Phenylalanine; Aib= 2-Aminoisobutyric acidSyntheticNOP-Receptor ligands37 °C for 240 min6 μg/μl11.3 ±1.4Mouse brain homogenate proteasesRP-HPLCMouse brain homogenatein vitro20497197NoneHypotensive and bradycardic effects evoked by UFP-112 after i.v. administration in rats wast lasting for (i.e. 80 min
2633
186978652008
GSSFLSPEHQRVQQRKESKKPPAKLQPR
Ghrelin28FreeFreeLinearLn-octanoyl group at ser 3Secreted by stomach P/D1-type cellsStimulates apetite and GH secretionBlood collected after 20 minutes to 2200 h after i/v injection of peptide1 µg/kg i/v injected21 ±3.0Human plasma proteasesCompetitive RadioimmunoassayHuman plasmain vivo15788704NoneNot reported
2634
186978652008
GSSFLSPEHQRVQQRKESKKPPAKLQPR
Ghrelin28FreeFreeLinearLn-octanoyl group at ser 3Secreted by stomach P/D1-type cellsStimulates apetite and GH secretionBlood collected after 20 minutes to 2200 h after i/v injection of peptide3 µg/kg i/v injected45Human plasma proteasesCompetitive RadioimmunoassayHuman plasmain vivo15788704NoneNot reported
2635
189728372008
CSNLSTCVLGKLSQELHKLQTYPRTNTGSGTP
sCT (Salmon calcitonin)32FreeFreeCyclic (C1-C7)LNoneHormone secreted by the parafollicular cells of thethyroid gland Calcitropic Hormone, reduce blood calcium5-360minutes10 µM13.18Rat kidney homogenates proteasesLC-ESI-MSRat kidney homogenatesin vitroNoneNoneNot reported
2636
189728372008
CSNLSTCVLGKLSQELHKLQTYPRTNTGSGTP
sCT (Salmon calcitonin)32FreeFreeCyclic (C1-C7)LNoneHormone secreted by the parafollicular cells of thethyroid gland Calcitropic Hormone, reduce blood calcium5-360minutes10 µM43.07Rat kidney homogenates proteasesLC-ESI-MSRat Liver homogenatesin vitroNoneNoneNot reported
2637
197700152009
AEIYNKDGNKLDLYG
VrAPI (Aspartic protease inhibitor in seeds of V. radiata)15FreeFreeLinearLNoneFrom plant Vigna radiataProtease inhibitorpH 2-10, Temp 20-100 °C2mg -5mg at pH 3 and temperature 100~30NoneBradford assayBufferin vitroNoneNoneTotal (aspartic protease) activity 2516 U
2639
211851602011
VDKPPYLPRPRPPRRIYNR
O-1(Oncocin)19FreeAmidationLinearLNone2kDa Oncopeltus peptide derivativesAntimicrobial30-480 Minutes7.5 μg/100μl25 ±4Mouse serum proteasesMALDI-TOF-MSFull mouse serumin vivoNoneNoneMIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus
2652
211851602011
VDKPPYLPRPRPPRrIYNR
O-16 (Oncocin)19FreeAmidationLinearMixD-Arg at 15th position2kDa Oncopeltus peptide derivativesAntimicrobial30-480 Minutes7.5 μg/100μl58 ±2Mouse serum proteasesMALDI-TOF-MS25% mouse serumin vivoNoneNoneMIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus
2653
211851602011
VDKPPYLPRPRPPR-Har-IYN-Har
O-17 (Oncocin)19FreeAmidationLinearLHar=Homoarginine2kDa Oncopeltus peptide derivativesAntimicrobial30-480 Minutes7.5 μg/100μl55Mouse serum proteasesMALDI-TOF-MSFull mouse serumin vivoNoneNoneMIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus
2662
221868722011
DRVYIHPFHL
Angiotensin I10FreeFreeLinearLNoneDerived from angiotensinogenPrecursor of angiotensin-IIRoom Temperature1mg/mL1Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2663
221868722011
RPPGFSPFR
Bradykinin9FreeFreeLinearLNoneEndogenous peptide of kinin familyVasodilator, Inflammatory mediatorRoom Temperature1mg/mL<5Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2664
221868722011
YGGFMTSEKSQTPLVTLFKNAIIKNAYKKGE
β-Endorphin31FreeFreeLinearLNoneEndogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. Agonist of the opioid receptorsRoom Temperature1mg/mL<5Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2665
221868722011
YGGFL
[Leu5]Enkephalin5FreeFreeLinearLNoneEndogenous opioid neuropeptide in neurons of both the central and peripheral nervous system.NeurotransmitterRoom Temperature1mg/mL<5Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2666
221868722011
RPKPQQFFGLM
Substance P11FreeAmidationLinearLNoneMember of the tachykinin neuropeptide family.NeurotransmitterRoom Temperature1mg/mL10Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2668
221868722011
AGCKNFFWKTFTSC
Somatostatin14FreeFreeCyclic (C3-C14)LNoneNeuropeptide secreted by HypothalamusInhibits insulin and glucagon secretion.Room Temperature1mg/mL10Hydolytic activity of bacterial strain B-9HPLC and LC/ITMSBacterial strain B-9 cell culturein vitroNoneNoneNot reported
2670
222639692012
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP-Fc (Atrial natriuretic peptide- Fc)28FreeFreeCyclic (C7-C23)LNoneSynthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation.Natriuretic and vasodilator4-72 hours0.5mg/kg of protein2 to 5Rat plasma proteasesELISAFemale Wistar rats Plasmain vivoNoneNoneNot reported
2675
233185022013
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1(7 €“36)NH2 [Glucagon-like peptide-1]30FreeAmidationLinearLNoneGLP-1Regulate blood glucoseBlood sample collected after 32-60 minutes after the infusion of peptide20pmol/kg4.8 ±0.8Pig kidneys proteasesRadioactivity measurementPig kidneyin vivoNoneNoneNot reported
2676
233185022013
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Ex-4 (Exendin-4)39FreeFreeLinearLNoneDerived from Saliva of Gila monsterGLP-1 receptor agonistBlood sample collected after 50-130 minutes after the infusion of peptide10 pmol/kg32.8 ±4.1Pig kidneys proteasesRadioactivity measurement(Bolus injection)Pig kidneyin vivoNoneNoneNot reported
2677
233185022013
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Ex(1 €“30) or Exendin(1 €“30)30FreeFreeLinearLNoneSynthetic derived from Exendin 4GLP-1 receptor agonistBlood sample collected after 42-130 minutes after the infusion of peptide20 pmol/kg28.4 ±1.7Pig kidneys proteasesRadioactivity measurement(Bolus injection)Pig kidneyin vivoNoneNoneNot reported
2678
233185022013
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRPSSGAPPPS
GLP-1Arg34(7 €“36), Ex(31 €“39) or [GLP-Ex]39FreeFreeLinearLNoneSyntheticGLP-1 receptor agonistBlood sample collected after 42-130 minutes after the infusion of peptide20 pmol/kg19.5 ±3.3Pig kidneys proteasesRadioactivity measurement(Bolus injection)Pig kidneyin vivoNoneNoneNot reported
2679
238133022013
Sar-RVYIHPa
TRV0278Sar=SarcosineFreeLinearMixD-Ala at 8th positionSynthetic β-arrestin-biased agonistBeta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitmentNot mentioned0.01 - 20 μg/kg/min dose<2 (intial half life)Human plasma proteasesLC/MS/MSHuman plasmain vivoNoneNoneNot reported
2680
238133022013
Sar-RVYIHPa
TRV0278Sar=SarcosineFreeLinearMixD-Ala at 8th positionSynthetic β-arrestin-biased agonistBeta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitmentNot mentioned0.01 - 20 μg/kg/min dose~ 10 (Terminal half life)Human plasma proteasesLC/MS/MSHuman plasmain vivoNoneNoneNot reported
2683
245883432014
EGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1(9-36)(Glucagon Like protein-1)28FreeAmidationLinearLNoneGlucagon Like protein-1 (GLP-1)Vasodialator2-120 minutes20μg/Kg0.05Dog hepatocyte proteasesLC-MSMale beagle dog plasma (Dose i/v injected)in vivoNoneNoneNot reported
2684
245883432014
EGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1(9-36)(Glucagon Like protein-1)28FreeAmidationLinearLNoneGlucagon Like protein-1 (GLP-1)Vasodialator3-120 minutes50μg/Kg0.54Dog hepatocyte proteasesLC-MSMale beagle dog plasma (Dose s/c injected)in vivoNoneNoneNot reported
2685
245883432014
EGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1(7-36)(Glucagon Like protein-1)28FreeAmidationLinearLNoneGlucagon Like protein-1 (GLP-1)Vasodialator4-120 minutes50μg/Kg2.1Dog hepatocyte proteasesLC-MSMale beagle dog plasma (Dose s/c injected)in vivoNoneNoneNot reported
2686
250256262014
MKFTLFSVLVVLLIATFVAADDCPRICTADFRPVCGTPSGGRRSANRTFGNQCSLDSHNCLNKGDTYDKLHDGECK
Vasotab TY76FreeFreeLinearLNoneSalivary glands of the horsefly ofTabanus yaoVasodialator and anti-thrombic1-480 minutes5mg/kg>1Mouse plasma proteasesELISAKunming Mouse plasma (Dose i/v injected)in vivoNoneNoneAt the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively.
2687
250256262014
MKFTLFSVLVVLLIATFVAADDCPRICTADFRPVCGTPSGGRRSANRTFGNQCSLDSHNCLNKGDTYDKLHDGECK
Vasotab TY76FreeFreeLinearLNoneSalivary glands of the horsefly ofTabanus yaoVasodialator and anti-thrombic1-480 minutes5mg/kg50Mouse lungs proteasesELISAKunming Mouse lungs (Dose i/v injected)in vivoNoneNoneAt the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively.
2688
250393582014
EGTFTSDVSSYLEGQAAKEFIAWLVKGR
Gly8-GLP-1(7-36)(Glucagon Like protein-1)30FreeAmidationLinearLNoneGlucagon Like protein-1 (GLP-1)Vasodialator37 °C for 2-72 hours1000ng/ml0.6Rat plasma proteasesLC-MS/MSRat Plasmain vitroNoneNoneGLP-1 receptor Activation potency with EC50 = 8.3 ± 0.4 pM in HEK-293 cells
2707
252436352014
HAEGTFTSDVSCYLEGQAACEFIAWLVKGRG
GLP-1(Glucagon Like protein-1)31FreeFreeLinearLNoneGlucagon Like protein-1 (GLP-1)Antihyperglycemic5-90 hours500μg<2DPP IVELISADPP IVin vitroNoneNoneThe insulin levels were increased dramatically to 806.74 ± 30.60 pmol/L within 15 min after GLP-1 administration
2715
257710002015
HSDAVFTDNYTRLRKQVAAKKYLQSIKNKRY
BAY55-9837 (VPAC2 receptor agonist)31FreeFreeLinearLNonePituitary adenylate cyclase-activating peptides (PACAPs) derived peptideInsulin secretion stimulant37 C, 48 Hours10 µM4.18Fxa(Facor Xa) and DPP-IVHPLC-ESI/MS/MSProtein Sample +HAS + Fxa +DPP IVin vitroNoneNoneAUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control
2716
257710002015
HSDAVFTDNYTRLRKQVAAKKYLQSIKNKRY
BAY55-9837 (VPAC2 receptor agonist)31FreeFreeLinearLNonePituitary adenylate cyclase-activating peptides (PACAPs) derived peptideInsulin secretion stimulant0.5-24 hours0.5 mg/kg~ 5db/db mice plasma proteasesLC-MS/MSdb/db Mice plasma (Dose i/v injected)in vivoNoneNoneAUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control
2717
257710002015
HSDAVFTDNYTRLRKQVAAKKYLQSIKNKRY
BAY55-9837 (VPAC2 receptor agonist)31FreeFreeLinearLNonePituitary adenylate cyclase-activating peptides (PACAPs) derived peptideInsulin secretion stimulant0.5-24 hours0.5 mg/kg~ 5Rabbit plasma proteasesLC-MS/MSNew Zealand White Rabbit plasma (Dose i/v injected)in vivoNoneNoneAUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control
2735
261979312015
YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY(3-34) [Peptide YY]34FreeFreeLinearLNoneSynthetic peptide hormone released from enteroendocrine cellsAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Blood sample collected after 15minutes of the infusion of peptide100 pmol/kg3.6 ±0.5Pig blood proteasesRadioimmunoassayFemale pigs bloodin vivoNoneNonePorcine PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.9nmol/L
2736
261979312015
YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY(1-36) [Peptide YY]36FreeFreeLinearLNoneSynthetic peptide hormone released from enteroendocrine cellsAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Blood sample collected after 15minutes of the infusion of peptide100 pmol/kg7.3 ±0.8Pig blood proteasesRadioimmunoassayFemale pigs bloodin vivoNoneNoneNot reported
2751
262221802015
HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGRG
G 37 or [GLP-1(7 €“37)]31FreeFreeLinearLNoneGlucagon-like peptide 1 (GLP-1)Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Room Temp0.4 µM1 ±0.3Human blood proteases + DPP IVMSEDTA whole bloodin vitroNoneNoneNot reported
2763
263080952015
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneSaliva of Gila monsterRegulates blood glucose by upregulating the insulin secretionBlood sample collected after 1-96 hours after the injection of peptide5nmol/Kg30Rat plasma proteasesELISA, LC/MSRat Plasma (Dose i/v injected)in vivoNoneNoneNot reported
2768
263253232015
pGlu-HWSYGLRPG
Endogenous LHRH10FreeAmidationLinearLPyro-Glutamate at 1st positionHypothalamusStimulates pitutiary gland to secretes to release gonadotropins(LH, FSH)Blood sample collected after0.5-24 hours after the injection of peptide2.5mg/Kg4-8minHuman plasma proteasesLC/MSHuman plasma (Dose s/c injected)in vivoNoneNoneNot reported
2771
263372312015
LLTHTISRIAVSYQTKVNLL
P16 [TNF α (75 €“94)]20FreeFreeLinearLNoneTumor necrosis factor-derived (TNF)Tumor growth inhibitor and anti-angiogenicBlood sample collected after0.5-24 hours after the injection of peptide5mg/kg0.096 ±0.008BALB/c mice plasma proteasesLC/MSBALB/c mice plasma (Dose i/v injected)in vivoNoneNoneGrowth inhibition effect of RMP16 was observed in DU145 cells (IC50 = 17.20 ± 1.95 nM, Tumor inhibition rates of P16-treated mice was 21.81%
2773
264000222015
fPRPGGGGQGDFEEIPEEYL
Hirulog-120FreeFreeLinearMixNoneHirudin derivedAnti-coagulantNot mentioned1.0μM/Kg20-25Human plasma proteasesHPLC, MS-MSHuman plasma (Dose i/v injected)in vivoNoneNoneInhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM
2774
264000222015
fPRPGGGGQGDFEEIPEEYL
Hirulog-120FreeFreeLinearMixNoneHirudin derivedAnti-coagulantNot mentioned1.0μM/Kg15 ±1.3Rat plasma proteasesHPLC, MS-MSSprague-Dawley (SD) rats plasma (Dose i/v injected)in vivoNoneNoneInhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM
2775
264000222015
fPRPGGGGQGDFEPIPEDAYDE
Peptide 1 (Hirudin mimetic peptide)22FreeAmidationLinearMixNoneHirudin derivedAnti-coagulantNot mentioned1.0μM/Kg13+-2.6Rat plasma proteasesHPLC, MS-MSSprague-Dawley (SD) rats plasma (Dose i/v injected)in vivoNoneNoneInhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 13.40 ± 0.46 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 5.80 ± 0.55nM
2777
186328262008
CKQSCSFGPFTFVCDGNTK
99m Tc-Duramycin19FreeFreeLinearLSuccinimidyl 6-hydrazinonicotinate acetone hydrazone (HYNIC) derivatized, HYNIC conjugated at either at Cys -1 or Amine group Of Lys-2Phosphatidylethanolamine binding probe and employed in In Vivo Imaging of Acute Cardiac Cell DeathMolecular probe for imaging PtdEBlood sample collected at 1-60 minutes2.3nmol<4Rat blood proteasesHPLC radiodetection (radio-HPLC)Healthy Sprague €“Dawley rats bloodin vivoNoneNoneBinding of 99mTc-duramycin to apoptotic cells was elevated by a factor of 32 ± 6
2778
214590962011
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneDerived from parotid glandVasorelaxing37 °C for 0-125 minutesNot mentioned1.3Human kidney proteasesNot mentionedHuman kidney membrane extractin vitroNoneNoneNot reported
2779
214590962011
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
BNP(B-type natriuretic peptide)32FreeFreeCyclic (C10-C26)LNoneBrain natriuretic peptideCardiac fibrosis Inhibitor37 °C for 0-125 minutesNot mentioned8Human kidney proteasesNot mentionedHuman kidney membrane extractin vitroNoneNoneNot reported
2780
214590962011
GLSKGCFGLKLDRIGSMSGLGC
CNP(C-type natriuretic peptide)22FreeFreeCyclic (C6-C22)LNoneSecreted from vascular endotheliumVasodialator37 °C for 0-125 minutesNot mentioned4.3Human kidney proteasesNot mentionedHuman kidney membrane extractin vitro19395584NoneNot reported
2782
214590962011
GLSKGCFGLKLDRIGSMSGLGCPSLRDPRPNAPSTSA
CD-NP (C-terminal tail of DNP)37FreeFreeCyclic (C6-C22)LNoneChimeric peptide derived from CNP and DNPNatriuretic and aldosterone suppressor37 °C for 0-125 minutesNot mentioned17-22.9Human kidney proteasesNot mentionedHuman kidney membrane extractin vitroNoneNoneNot reported
2784
193446732009
SCSlPQT
Mouse [D-Leu-4]OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerBlood collected after 5-120 minutes after peptide delivery1mg/200ul30Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intraperitoneal route of delivery)in vivo11495687NoneNot reported
2785
193446732009
SCSlPQT
Mouse [D-Leu-4]OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerBlood collected after 5-120 minutes after peptide delivery1mg/200ul35Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Subcutaneous Route of delivery)in vivo11495687NoneNot reported
2786
193446732009
SCSlPQT
Mouse [D-Leu-4]OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerBlood collected after 5-120 minutes after peptide delivery1mg/200ul42Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intra-muscular route of delivery)in vivo11495687NoneNot reported
2787
193446732009
SCSlPQT
Mouse [D-Leu-4]OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerBlood collected after 5-120 minutes after peptide delivery1mg/200ul41.1Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intranasal route of delivery)in vivo11495687NoneNot reported
2788
191574212009
GPE
Glypromate3FreeFreeLinearLNoneN-terminal cleavage product of human insulin-like growth factor-1 (IGF-1) in the brainNeuroprotectiveBlood collected after 0.5-12 hours after peptide delivery3 -10 mg/kg/h dose5Rat plasma proteasesLC-MSSprague-Dawley rats plasma (Dose i/v injected)in vivoNoneNoneNot reported
2789
191574212009
GPE
NNZ-2566 (Glycyl-L-2-methylprolyl-L- glutamic acid)3FreeFreeLinearLMethylation of alpha-C of ProGlypromate analogueNeuroprotectiveBlood collected after 0.5-12 hours after peptide delivery3 -10 mg/kg/h dose49Rat blood proteasesLC-MSSprague-Dawley rats brain (Dose i/v injected)in vivoNoneNoneNNZ-2566-treated animals(i/v) exhibited an average infarct area of 79.8 ±10.4 mm2 (3 mg/kg/h, pb0.01) and 21.3 ±7.5 mm2 (10 mg/kg/h) as compare to ET-1 induced an infarct area of 153.1 ±20.1 mm2 (mean ±s.e.m) in saline-treated rat; Total injury size was 22.2 ±5.7 mm2 following 30 mg/kg (76% protection; Dunnett's multiple comparison test) and only 4.6 ±2.3 mm2 following 60 mg/kg (95% protection; Dunnett's multiple comparison test).
2797
241398442013
Hyp-AS-Chg-Q
Conjuagte 3(conjugates of 4-aminocyclophosphamide (4-NH2-CPA))5Bn-glutarylationAmidated CPALinearLNoneSynthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA)Anti-cancerNot mentionedNot mentioned55PSA(Prostate-specific antigen )HPLCConjuagte 3+PSA(Prostate-specific antigen)in vitroNoneNonepEC50-8.19 ±1.0minutes, Emax 9.44 ±0.3 nmol/well
2799
248747042014
YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
AM(adrenomedullin)52FreeAmidationCyclic (Ringed structure formed by C16-C21)LNoneIsolated from Human pheochromocytomaVasodilator and cardiovascular protectionNot mentioned3nmol/kg Dose15.2 ±1.9 min (2nd plasma half life)Rat plasma proteasesELISAMale Wistar rats plasmain vivohttp://www.genscript.com/peptide/RP11288-AdrenomedNoneNative human AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.59 ± 0.90 and9.30 ± 0.26 nmol/well
2800
248747042014
YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
PEGylated AM52PegylationAmidationCyclic (Ringed structure formed by C16-C21)LNoneIsolated from Human pheochromocytomaVasodilator and cardiovascular protectionNot mentioned3nmol/kg Dose4.87 ±0.68(1st plasma half life)Rat plasma proteasesELISAMale Wistar rats plasmain vivohttp://www.genscript.com/peptide/RP11288-AdrenomedNonePEGylated AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.519 ± 0.10 and9.44 ± 0.30 nmol/well
2807
254539792014
SCSlPQT
(D-Leu-4)OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerNot mentionedPeptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio34Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum(Subcutaneous Route of delivery)in vivoNoneNoneEfficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2808
254539792014
SCSlPQT
(D-Leu-4)OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerNot mentionedPeptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio49Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intraperitoneal route of delivery)in vivoNoneNoneEfficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2809
254539792014
SCSlPQT
(D-Leu-4)OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerNot mentionedPeptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio36Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intra-muscular route of delivery)in vivoNoneNoneEfficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2810
254539792014
SCSlPQT
(D-Leu-4)OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerNot mentionedPeptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio20Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Oral route of delivery)in vivoNoneNoneEfficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM
2811
254539792014
SCSlPQT
(D-Leu-4)OB37FreeFreeLinearMixNoneSynthetic peptide amide with leptin-like activityRegulate energy balance by inhibiting hungerNot mentionedPeptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio41Mice serum proteasesCompetitive ELISAMale Swiss Webster mice serum (Intranasal route of delivery)in vivoNoneNoneStimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS
2812
244628992014
CSSPIQGSWTWENGK(propargylglycine)WTWKGIIRLEQ
APTEDB-DTX (Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate)27FreeFreeLinearLModified Gly at 16th postion i.e. propargylglycine and peptide conjugated with drug DTX at this positionFibronectin extra domain B (EDB)-specific aptide docetaxel conjugateDrug(anticancer agent i.e. DTX) Delivery vehicleNot mentioned5 mg DTX/kg Dose0.491Mice serum proteasesHPLCC57BL6 mice Serumin vivoNoneNoneStimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS
2813
50922902014
LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES
LL-37 (Antimicrobial Peptide)37FreeFreeLinearLNoneHuman epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein)Antimicrobial15-720 minutes hour3 µM~1CathepsinProteolysis assay, (confirmed by Western blotting)Western Blottingin vitro16716248NoneNot reported
2816
13194551992
SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII
hCRH(Human Corticotropin Releasing Hormone)41FreeFreeLinearLNoneDerived from Pre-hormoneHormone causes Adrenocorticotropin secrection and neurotransmitter2.5-180 minutes100μg30.5 ±3.3Human plasma proteasesIRM(Immunoradiometric assays)Human plasmain vivo12379493None22.4 ± 8.1 ng/hour (ACTH response)
2817
13194551992
SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII
hCRH(Human Corticotropin Releasing Hormone)41FreeFreeLinearLNoneDerived from Pre-hormoneHormone causes Adrenocorticotropin secrection and neurotransmitter2.5-180 minutes100μg46.5 ±7.2Sheep plasma proteasesIRM(Immunoradiometric assays)Human plasmain vivo12379493None46.5 ± 6.4 ng/hour (ACTH response)
2818
13194551992
SQEPPISLVLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
oCRH(Ovine Corticotropin Releasing Hormone)41FreeFreeLinearLNoneDerived from Pre-hormoneHormone causes Adrenocorticotropin secrection and neurotransmitter2.5-180 minutes100μg42.8 ±6.4Human plasma proteasesIRM(Immunoradiometric assays)Sheep plasmain vivo6603620None39.9 ± 11.7 ng/hour (ACTH response)
2819
13194551992
SQEPPISLVLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
oCRH(Ovine Corticotropin Releasing Hormone)41FreeFreeLinearLNoneDerived from Pre-hormoneHormone causes Adrenocorticotropin secrection and neurotransmitter2.5-180 minutes100μg39.8 ±10.1Sheep plasma proteasesIRM(Immunoradiometric assays)Sheep plasmain vivo6603620None40.2 ± 8.4 ng/hour (ACTH response)
2826
13876081992
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneHormone secreted by heart muscle cellsNatriuretic and vasodilatorBlood collected 1-60 minutes after peptide infused2μg/min12.5 (Terminal half life)Human plasma proteasesIRM(Immunoradiometric assays)Young Human plasma (average age 23.3) (Dose i/v injected)in vivoNoneNoneNot reported
2827
13876081992
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneHormone secreted by heart muscle cellsNatriuretic and vasodilatorBlood collected 1-60 minutes after peptide infused2μg/min9.6 (Terminal half life)Human plasma proteasesIRM(Immunoradiometric assays)Older Human plasma(average age 75.3) (Dose i/v injected)in vivoNoneNoneNot reported
2835
16464651991
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
rANP(99-126) (Recombinant atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneDerived from ANP (Atrial natriuretic peptide)Natriuretic and vasodilatorBlood samples collected at 5-1800 seconds after peptide injecteionNot mentioned114 ±38.6Rat plasma proteasesRadioimmunoassayMale Wistar rats plasmain vivoNoneNoneNot reported
2836
16464651991
SQDSAERIQERLRNSKMAHSSSCFGQKIDRIGAVSRLGCDGLRQF
iso-rANP(1-45) (Recombinant atrial natriuretic peptide)45FreeFreeCyclic (C23-C39)LNoneDerived from ANP (Atrial natriuretic peptide)Natriuretic and vasodilatorBlood samples collected at 5-1800 seconds after peptide injecteion1 x 106 cpm130 ±13Rat plasma proteasesRadioimmunoassayMale Wistar rats plasma (Dose i/p injected)in vivoNoneNoneNot reported
2838
16464651991
SQDSAERIQERLRNSKMAHSSSCFGQKIDRIGAVSRLGCDGLRQF
iso-rANP(1-45) (Recombinant atrial natriuretic peptide)45FreeFreeCyclic (C23-C39)LNoneDerived from ANP (Atrial natriuretic peptide)Natriuretic and vasodilatorBlood samples collected at 5-1800 seconds after peptide injecteion1x 106 cpm164.3 ±9.0(β- t1/2)Rat plasma proteasesRadioimmunoassayMale Wistar rats plasma (Dose i/p injected)in vivoNoneNoneNot reported
2841
16497281991
HSDAVFTDNYTRLRKQMAVKKYLNSILN
VIP(Vasoactive intestinal peptide)28FreeAmidationLinearLNonePeptide hormone secreted by IntestineStimulates the secretion of electrolytes and waterSample collected at 40-50 minutes10pmol min-1 kg -1 peptide infused1.27 ±0.20Rabbit plasma proteasesRadioimmunoassayNew Zealand White rabbits plasma(have normal sodium diet i.e. 29.35 k 4.02 pmol/l)in vivoNoneNoneNot reported
2843
17236381991
GWTLNSAGYLLGPHAI
Galanin(1-16)16FreeFreeLinearLNoneHigh affinity synthetic agonistNeuroendocrine activities, stimulates growth hormone secretion37 °C2 μM28Hypothalamic membrane protaesesHPLCHypothalamic membranes of Male Sprague-Dawley ratsin vitroNoneNoneNot reported
2844
17308071992
HwAWfK
GHRP (Growth Hormone releasing peptide)6FreeAmidationLinearMixNoneGrowth Hormone releasing peptideRelease growth hormoneNot mentioned100μg/kg20Human serum proteasesRadioimmunoassayHuman serumin vivoNoneNoneGH response elicited by 300 μg/kg on oral administeration of peptide
2845
17631931991
aSTTTNYT
Peptide T (Dala1-peptide T-NH2)8FreeAmidationLinearMixNoneSynthetic derived from the external envelope protein of HIV IIIBHIV-entry inhibitorNot mentionedIntravenous test dose of 0.033 mg/Kg of peptide T30-60AIDS patient plasma proteasesRadioimmunoassay , HPLCAIDS patient plasmain vivoNoneNoneNot reported
2846
18266671991
YADAIFTNSYRKVLGQLSARKLLQDIMSR
GRF(1-29)-NH2 (Growth hormone-releasing factor (GRF- Growth regulating factor))29FreeAmidationLinearLNoneGrowth regulating factor (GRF)Release growth hormoneNot mentioned100 µg/ml0.25Porcine plasma proteasesHPLCPorcine plasmain vitroNoneNoneNot reported
2847
18266671991
YADAIFTNSYRKVLGQLSARKLLQDIMSR
[Ala15]GRF(1-29)-NH229FreeAmidationLinearLNoneSynthetic(GRF-1 analogs)Release growth hormoneNot mentioned100 µg/ml0.3Porcine plasma proteasesHPLCPorcine plasmain vitroNoneNoneNot reported
2848
18266671991
YADAIFTNSYRKVLGQLSARKLLQDIMSR
[DesNH2-Tyr1,Ala15]GRF(1-29)-NH229Chlorpheniramine MAmidationLinearLNoneSynthetic(GRF-1 analogs)Release growth hormoneNot mentioned100 µg/ml1Porcine plasma proteasesHPLCPorcine plasmain vitroNoneNoneNot reported
2849
18266671991
YaDAIFTNSYRKVLAQLSARKLLQDIMSR
[DesNH2-Tyr1,D-Ala2,Ala15]GRF(1-29)-NH229Chlorpheniramine MAmidationLinearMixNoneSynthetic(GRF-1 analogs)Release growth hormoneNot mentioned100 µg/ml1Porcine plasma proteasesHPLCPorcine plasmain vitroNoneNoneNot reported
2855
18891241991
AQKVNSGEPRAHLGALLARYIQQARKAPSGRMSVIKNLQNLDPSHRISDRDYMGWMDF
CCK58 (Cholecystokinin 58)58FreeAmidationLinearLNone Peptide hormone of the gastrointestinal systemStimulates digestion of fat & protein37 °C for 30-180 minutes1.6pmol45 ±5Normal Human plasma proteasesRadioimmunoassay and HPLCNormal Human plasmain vitroNoneNoneNot reported
2857
18891241991
AQKVNSGEPRAHLGALLARYIQQARKAPSGRMSVIKNLQNLDPSHRISDRDYMGWMDF
CCK58 (Cholecystokinin 58)58FreeAmidationLinearLNone Peptide hormone of the gastrointestinal systemStimulates digestion of fat & protein37 °C for 30-180 minutes1.6pmol10.4 ±1.1Pancreatitis patients blood proteasesRadioimmunoassay and HPLCPancreatitis patient plasmain vitroNoneNoneNot reported
2858
18891241991
AQKVNSGEPRAHLGALLARYIQQARKAPSGRMSVIKNLQNLDPSHRISDRDYMGWMDF
CCK58 (Cholecystokinin 58)58FreeAmidationLinearLNone Peptide hormone of the gastrointestinal systemStimulates digestion of fat & protein37 °C for 30-180 minutes1.6pmol11.1 ±1Pancreatitis patients plasma proteasesRadioimmunoassay and HPLCPancreatitis patient bloodin vitroNoneNoneNot reported
2864
21622751990
HADGVFTSDFSKLLGQLSAKKYLESLM
PHM (Peptide histidine methionine)27FreeAmidationLinearLNonePeptide derived from Prepro-VIPVasodilatorNot mentioned5 pmol min-1 kg-16.5Human plasma proteasesRadioimmunoassayHuman plasmain vivoNoneNoneIt increase heart rate
2865
21622751990
HADGVFTSDFSKLLGQLSAKKYLESLMGKRVSSNISEDPVPV
PHV (Peptide histidine valine)42FreeFreeLinearLNonePeptide derived from Prepro-VIPVasodilatorNot mentioned5 pmol min-1 kg-137.5Human plasma proteasesRadioimmunoassayHuman plasmain vivoNoneNoneIt increases heart rate but not significantly
2866
28963431988
YADAIFTNSYRKVLGQLSARKLLQDIMSR
GRF(1-29)-NH2 (Growth regulating factor)29FreeAmidationLinearLNoneGrowth regulating factorRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl6.2 ±0.7Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 100%
2867
28963431988
YaDAIFTNSYRKVLGQLSARKLLQDIMSR
[D-Ala2]-GRF(1-29)-NH2 (Growth regulating factor)29FreeAmidationLinearMixNoneGRF-1 analogsRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl6.6 ±0.4Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 5146%
2868
28963431988
YAdAIFTNSYRKVLGQLSARKLLQDIMSR
[D-Asp3]-GRF(1-29)-NH2 (Growth regulating factor)29FreeAmidationLinearMixNoneGRF-1 analogsRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl5.9 ±0.8Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 670%
2869
28963431988
YADAIFTnSYRKVLGQLSARKLLQDIMSR
lD-Asn8]-GRF(1-29)-NH2 (Growth regulating factor)29FreeAmidationLinearMixNoneGRF-1 analogsRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl6.9 ±0.5Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 221%
2870
28963431988
YADAIFTNSyRKVLGQLSARKLLQDIMSR
[D-Tyr10]-GRF(1-29)-NH2 (Growth regulating factor)29FreeAmidationLinearMixNoneGRF-1 analogsRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl4.7 ±0.8Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 230%
2871
28963431988
yaDAIFTNSYRKVLGQLSARKLLQDIMSR
Ac-[D-Tyr1,D-AIa2]GRF(1-29)-NH2 (Growth regulating factor)29AcetylationAmidationLinearMixNoneGRF-1 analogsRelease growth hormoneBlood collected 1-90 minutes after peptide injection20μg/200μl7.4 ±0.5Rat plasma proteasesRadioimmunoassayRat plasma (i/v and s/c route of injection)in vivoNoneNoneRelative potency for GH releasing activity = 2817%
2872
29406251986
pyr-EHWSYwLRPG
[D-Trp6]-LHRH (Luteinizing hormone-releasing hormone)10FreeAmidationLinearMixPyr=Pyro-glutamic acidLHRH (Luteinizing hormone-releasing hormone) derivativeRelease Luteinizing hormoneBlood collected 1-240 minutes after peptide infused100 µg/ml>10 (alpha t1/2)Dog plasma proteasesHPLCTwo male Beagle dogs plasma (Dose s/c injected)in vivoNoneNoneNot reported
2880
29535161987
RRSSCFGGRMDRIGAQSGLGCNSFRY
rANP (Recombinant Atrial natriuretic peptide )26FreeFreeCyclic (C5-C21)LNoneAtrial natriuretic factorNatriuretic, diuretic and vasorelaxant peptideBlood collected 0.2-2 hours after peptide injection1 μg/min dose4.5Human plasma proteasesRadioimmunoassayHuman plasmain vivoNoneNoneANP induced dose-related effects on systemic and renal hemodynamic, as well as electrolyte excretion
2881
29663451988
NPVYSAVSNTDLMDFKNLLDHLEEKMPVEDEVMPPQALSEQTDEAGAALSSLSEVPPWTGEVNPSQRDGGALGRGPWDPSDRSALLKSKLRALLAGPR
rANF(Asn1-Arg98) [Rat atrial natriuretic factor]98FreeFreeLinearLRadioiodinated peptide at Tyr-4Rat ANF derivative [Rat atrial natriuretic factor]Natriuretic, diuretic and vasorelaxant peptideNot mentioned10 X106 CPM54.8 ±3.9(2nd component)Rat plasma proteasesRadioimmunoassayMale Sprague-Dawley rats plasmain vivohttp://www.uniprot.org/uniprot/P01161NoneNot reported
2882
29663451988
NPVYSAVSNTDLMDFKNLLDHLEEKMPVEDEVMPPQALSEQTDEAGAALSSLSEVPPWTGEVNPSQRDGGALGRGPWDPSDRSALLKSKLRALLAGPR
rANF(Asn1-Arg98) [Rat atrial natriuretic factor]98FreeFreeLinearLRadioiodinated peptide at Tyr-4Rat ANF derivative [Rat atrial natriuretic factor]Natriuretic, diuretic and vasorelaxant peptideNot mentioned10 X106 CPM2.5 ±0.3(1st compent)Rat plasma proteasesRadioimmunoassayMale Sprague-Dawley rats plasmain vivohttp://www.uniprot.org/uniprot/P01162NoneNot reported
2883
29889191985
SQEPPISLVLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
r/hCRF(Human/rat corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection10 µg/kg peptide injected to rhesus monkey4.0 ±1.2 (t1/2fast)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 1035 ± 226 %, cortisol increased by 123 ± 34% on 10 µg/kg dose
2884
29889191985
SQEPPISLVLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
r/hCRF(Human/rat corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection100 µg/kg peptide injected to rhesus monkey1.5 ±0.5 (t1/2fast)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose
2885
29889191985
SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII
oCRF(Ovine corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection1 µg/kg peptide injected to rhesus monkey3.6 ±1.1 (t1/2 fast)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose
2886
29889191985
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
r/hCRF(Human/rat corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection10 µg/kg peptide injected to rhesus monkey29.0 ±2.0(t1/2 slow)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 1858 ± 452 %, cortisol increased by 123 ± 28% on 10 µg/kg dose
2887
29889191985
SQEPPISLDLTFHLLREVLEMTKADQLAQQAHSNRKLLDIA
r/hCRF(Human/rat corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection100 µg/kg peptide injected to rhesus monkey32.7 ±10.1 (t1/2 slow)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose
2888
29889191985
SEEPPISLDLTFHLLREVLEMARAEQLAQQAHSNRKLMEII
oCRF(Ovine corticotropin-releasing factor)41FreeFreeLinearLNonePeptide hormone secreted by hypothalamus Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) Blood samples collected at 1-180 minutes after peptide injection1 µg/kg peptide injected to rhesus monkey44.3 +/= 6.7 (t1/2 slow)Rhesus monkey proteasesRadioimmunoassayRhesus monkey plasmain vivoNoneNoneACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose
2891
31479011988
HSQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNKNNIA
Oxyntomodulin37FreeFreeLinearLNoneSynthetic derived from proglucagon, identified in extracts from porcine small intestinal mucosaGLP-1-GCGR (glucagon) agonistBlood samples collected at 1-5 hourss after peptide injection100- 400ng/kg/h12 ±1Human plasma proteasesRadioimmunoassayHuman plasma (Dose i/v injected)in vivohttp://www.glucagon.com/oxyntomodulin.htmlNoneThe acid secretion increased during the first 90 rnin of pentagastrin infusion from 1 - 2 meq H+/15 rnin to a plateau of 5-6 meq H+/15 min
2892
32154831988
YGGFM
MET-enkephalin (Methionine-enkephalin)5FreeFreeLinearLNoneEnkephalinNeurotransmitter37 °C for 1-180 minutes300pg (pooled platelet-poor plasma)12.8Human plasma proteasesTLC (Thin-layer chromatography)Human plasmain vitroNoneNoneNot reported
2893
32154831988
YGGFL
LEU-enkephalin (Leucine-enkephalin)5FreeFreeLinearLNoneEnkephalinNeurotransmitter37 °C for 1-180 minutes300pg (pooled platelet-poor plasma)7Human plasma proteasesTLC (Thin-layer chromatography)Human plasmain vitroNoneNoneNot reported
2894
32617721988
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
hCGRP(Human Calcitonin gene-related peptide)37FreeAmidationCyclic (C2-C7)LNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxiaBlood collected-10 to 90 minutes after peptide infusion5pmol/kg3.6 ±0.3 (Half life of 1st phase)Sheep plasma proteasesRadioimmunoassay, RP-HPLCMerino-Corriedale cross ewes (sheep) plasmain vivoNoneNoneNot reported
2895
32617721988
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
hCGRP(Human Calcitonin gene-related peptide)37FreeAmidationCyclic (C2-C7)LNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxiaBlood collected-10 to 90 minutes after peptide infusion5pmol/kg13.6 ±1.0(Half life of 1st phase)Sheep plasma proteasesRadioimmunoassay, RP-HPLCMerino-Corriedale cross ewes (sheep) plasmain vivoNoneNoneNot reported
2898
33793521988
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
Reduced IGF-1(Free form) (Insulin-like growth factor-I)70FreeFreeLinearLLabelled with 125I, Disulphide bond is reducedBovine IGF-1Mediates growth and developmentBlood collected 10 minutes to 30 hours after peptide infusion10mM/L0.8Lamb plasma proteasesRadioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivityEight merino lambs plasmain vivoNoneNoneNot reported
2900
33793521988
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
S-CM IGF-1 (Insulin-like growth factor-I)70FreeFreeLinearLS-CM=S-carboxymethylatedBovine IGF-1Mediates growth and developmentBlood collected 10 minutes to 30 hours after peptide infusion10mM/L0.8-0.9Lamb plasma proteasesRadioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivityEight merino lambs plasmain vivoNoneNoneNot reported
2901
36012351987
YPSKPDNPGEDAPAEDMARYYSALRHYINLITRQRY
Porcine NPY (Neuropeptide Y)36FreeAmidationLinearLNoneNeuropeptideActs as a neurotransmitterBlood collected 1 to 90 minutes after peptide infusion06-10nM/kg~ 20 (20-28)Dog plasma proteasesRadioimmunoassaySix mongrel dogs plasma (Dose i/v injected)in vivoNoneNoneNot reported
2902
34927291986
YGGFM
MET-enkephalin (Methionine-enkephalin)5FreeFreeLinearLNoneEnkephalinNeurotransmitterBlood collected 5-60 minutes after peptide infused1-20mM<2Proteases from rhesus monkey plasmaRP-HPLCRhesus monkey plasmain vitroNoneNoneNot reported
2903
37687311986
WAGGDASGE
DSIP (Delta sleep inducing peptide)9FreeFreeLinearLNoneNeuropeptide secreted from hypothamusStress reliever, stimulates LH, somatostatinBlood collected 2-60 minutes after peptide injected0.1mg/Kg7.24 ±0.77Proteases from dog plasmaRadioimmunoassayMongrel dog plasma(Dose i/v injected)in vivoNoneNoneNot reported
2904
37687311986
AGGDASGE
des-Trp-DSIP8FreeFreeLinearLNoneDSIP analogueAnticarcinogenicBlood collected 2-60 minutes after peptide injected0.1mg/Kg7.55 ±0.52Proteases from dog plasmaRadioimmunoassayMongrel dog plasma(Dose i/v injected)in vivoNoneNoneNot reported
2905
37687311986
WAaGDASGE
D-Ala3-DSIP9FreeFreeLinearMixNoneDSIP analogueAnticarcinogenicBlood collected 2-60 minutes after peptide injected0.1mg/Kg8.19 ±0.30Proteases from dog plasmaRadioimmunoassayMongrel dog plasma(Dose i/v injected)in vivoNoneNoneNot reported
2906
37687311986
WAGaDASGE
D-Ala4-DSIP9FreeFreeLinearMixNoneDSIP analogueAnticarcinogenicBlood collected 2-60 minutes after peptide injected0.1mg/Kg12.9 ±0.83Proteases from dog plasmaRadioimmunoassayMongrel dog plasma(Dose i/v injected)in vivoNoneNoneNot reported
2907
37687311986
WAGaDASGE
D-Ala4-DSIP-NH29FreeAmidationLinearMixNoneDSIP analogueAnticarcinogenicBlood collected 2-60 minutes after peptide injected0.1mg/Kg10.2 ±0.69Proteases from dog plasmaRadioimmunoassayMongrel dog plasma(Dose i/v injected)in vivoNoneNoneNot reported
2908
39246851985
YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGA
hGRF-1(1-40) (Human growth regulating factor)40FreeAmidationLinearLNoneHuman growth regulating factorRelease growth hormoneBlood collected 60-240 minutes after peptide injection5 µg/200ul57.3 ±1.5 (beta or elimination half life)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivoNoneNoneNot reported
2909
39246851985
YADAIFTNSYRKVLGQLSARKLLQDIMSRQQGESNQERGA
hGRF-1(1-40) (Human growth regulating factor)40FreeAmidationLinearLNoneHuman growth regulating factorRelease growth hormoneBlood collected 60-240 minutes after peptide injection5 µg/200ul3.2 ±0.2 (alpha or distribution half life)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivoNoneNoneNot reported
2910
15514971992
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide (Connecting peptide)31FreeFreeLinearLNonePro-insulin derivativeConnect A- and B-chains of insulin and regulates Ca-dependent cell signalingBlood collected 2-180 minutes after peptide injection150 µg of peptide injected4.95 ±1.04(short half life or initial decay)Proteases from Human plasmaRadioimmunoassayHuman plasmain vivoNoneNoneInsulin secretion rates can be accurately estimated from plasma levels of C-peptide
2911
15514971992
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide (Connecting peptide)31FreeFreeLinearLNonePro-insulin derivativeConnect A- and B-chains of insulin and regulates Ca-dependent cell signalingBlood collected 2-180 minutes after peptide injection150 µg of peptide injected32.4 ±5(long half life)Proteases from Human plasmaRadioimmunoassayHuman plasmain vivoNoneNoneInsulin secretion rates can be accurately estimated from plasma levels of C-peptide
2912
15514971992
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide (Connecting peptide)31FreeFreeLinearLNonePro-insulin derivativeConnect A- and B-chains of insulin and regulates Ca-dependent cell signalingBlood collected 2-180 minutes after peptide injection150 µg of peptide injected4.55 ±1.23 (short half life or initial decay)Proteases from Human(obese) plasmaRadioimmunoassayHuman(obese) plasmain vivoNoneNoneInsulin secretion rates can be accurately estimated from plasma levels of C-peptide
2913
15514971992
EAEDLQVGQVELGGGPGAGSLQPLALEGSLQ
C-peptide (Connecting peptide)31FreeFreeLinearLNonePro-insulin derivativeConnect A- and B-chains of insulin and regulates Ca-dependent cell signalingBlood collected 2-180 minutes after peptide injection150 µg of peptide injected32.4 ±5(long half life)Proteases from Human(obese) plasmaRadioimmunoassayHuman(obese) plasmain vivoNoneNoneInsulin secretion rates can be accurately estimated from plasma levels of C-peptide
2914
16517381991
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
alpha-ANP (alpha-atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNonealpha-atrial natriuretic peptideNatriuretic and vasodilatorBlood collected 30-60 minutes during and 5-20 minutes after peptide injection0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h4.3 ±0.6Proteases from Human plasma(younger, 20-39 years old)RadioimmunoassayHuman plasma(younger, 20-39 years old)in vivoNoneNoneNatriuresis (145 ±36 ν 142 ± 28 µMol/min) and urinary cGMP excretion (40.9 ± 6.7 nmol/h)
2915
16517381991
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
alpha-ANP (alpha-atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNonealpha-atrial natriuretic peptideNatriuretic and vasodilatorBlood collected 30-60 minutes during and 5-20 minutes after peptide injection0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h7.8 ±0.6Proteases from Human plasma(older, 65-83 years old)RadioimmunoassayHuman plasma(older, 65-83 years old)in vivoNoneNoneNatriuresis 142 ± 28 µMol/min and urinary cGMP excretion 35.3 ± 4.1
2916
17779641991
APGPR
CLAP(Prpcolipase activation peptide)5FreeFreeLinearLNoneDerived from colipaseProcolipase activation peptideRoom Temperature(25C)500nM/L5Proteases from Human serumELISAHuman Serumin vitroNoneNoneNot reported
2918
18312491991
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP(99-126) (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneHormone secreted by heart muscle cellsNatriuretic and vasodilatorBlood collected 2-20 minutes after peptide infused5pmol/kg4.8 ±0.8Proteases from Human plasma (Chronic renal diseases)RadioimmunoassayHuman plasma (Chronic renal diseases)in vivoNoneNoneGFR and ERPF increased by a mean value of 23% and 27% respectively
2919
18820911991
PGlu-HWSYGLRPG
GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearLpGlu= Pyro-glutamateHormone secreted by HypothalamusStimulates the release of the gonadotropins from the pituitary.37 °C40mg/ml10.5Proteases from Rat ovary tissuesRadioimmunoassayRat ovary tissuesin vitro1631133NoneNot reported
2920
18820911991
PGlu-HWSYGLRPG
GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearLpGlu= Pyro-glutamateHormone secreted by HypothalamusStimulates the release of the gonadotropins from the pituitary.37 °C40mg/ml45Proteases from Rat Lung tissuesRadioimmunoassayRat lung tissuesin vitro1631133NoneNot reported
2921
18820911991
PGlu-HWSYGLRPG
GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearLpGlu= Pyro-glutamateHormone secreted by HypothalamusStimulates the release of the gonadotropins from the pituitary.Blood collected 30-300 minutes after peptide injection24 µg/kg2.66 (t1/2 alpha)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivo1631133NoneNot reported
2922
18820911991
PGlu-HWSYGLRPG
GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearLpGlu= Pyro-glutamateHormone secreted by HypothalamusStimulates the release of the gonadotropins from the pituitary.Blood collected 30-300 minutes after peptide injection24 µg/kg12.16 (t1/2 beta)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivo1631133NoneNot reported
2924
18820911991
PGlu-HWSYfLRPG
D-Phe-6-GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearMixNoneGnRH derivativeStimulates the release of the gonadotropins from the pituitary.Blood collected 30-300 minutes after peptide injection24 µg/kg14.53Rat plasma proteasesRadioimmunoassay(Dose i/m injected)Rat plasmain vivo1631133NoneNot reported
2926
18820911991
PGlu-HwSYfLRPG
D-Trp3-D-Phe-6-GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearMixNoneGnRH derivativeStimulates the release of the gonadotropins from the pituitary.Blood collected 30-300 minutes after peptide injection24 µg/kg25.8 (t1/2 beta)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivo1631133NoneNot reported
2927
18820911991
PGlu-HwSYfLRPG
D-Trp3-D-Phe-6-GnRH (Gonadotropin releasing hormone)10FreeAmidationLinearMixNoneGnRH derivativeStimulates the release of the gonadotropins from the pituitary.Blood collected 30-300 minutes after peptide injection24 µg/kg36.4Rat plasma proteasesRadioimmunoassay(Dose i/m injected)Rat plasmain vivo1631133NoneNot reported
2928
21568861990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection2 pmol/kg peptide infused3.1Proteases from Human plasmaRadioimmunoassayHuman plasmain vivoNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2929
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection0.17-0.25 Mbeq peptide infused1.23 ±0.35Rat plasma proteasesHPLCRat plasmain vivoNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2930
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection0.17-0.25 Mbeq peptide+ captoril(ACE inhibitor) infused6.99 ±0.34Rat plasma proteasesHPLCRat plasmain vivoNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2931
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infused11.8 ±0.49Rat plasma proteasesHPLCRat plasmain vivoNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2932
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused14.3 ±0.48Rat plasma proteasesHPLCRat plasmain vivoNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2933
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection1.5 Kbeq peptide4.6 ±0.1Proteases from Rat serumHPLCRat Serumin vitroNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2934
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection1.5 Kbeq peptide+ captoril(ACE inhibitor8.3 ±0.3Proteases from Rat serumHPLCRat Serumin vitroNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2935
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infuse5.6 ±0.2Proteases from Rat serumHPLCRat Serumin vitroNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2936
21751781990
DSGCFGRRLDRIGSLSGLGCNVLRRY
Porcine 125I-BNP(1-26)26FreeFreeCyclic (C4-C20)LTyr is Iodinated (125I)Porcine brain and heartNatriuretic and vasodilatorBlood collected 2-270 minutes after peptide injection1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused9.9 ±0.4Proteases from Rat serumHPLCRat Serumin vitroNoneNonePRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP
2939
24548051988
FVNQHLCGSHVDELQYLCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
[125I]B-chain mutant IGF-171FreeFreeLinearLNoneHuman Recombinant peptideStmulates glycogen synthesisBlood collected 10 minutes to 6 hours after peptide injection2 µCi peptide injected to rhesus monkey27.5Proteases from Rat serumRadioimmunoassayRat Serumin vivoNoneNoneStimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm
2940
24548051988
GPQALCGAELVDALYLVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
[125I] [Gln3,Ala4,Tyr15,Leu16]IGF-170FreeFreeLinearLNoneHuman Recombinant peptideStmulates glycogen synthesisBlood collected 10 minutes to 6 hours after peptide injection3 µCi peptide injected to rhesus monkey26.9Proteases from Rat serumRadioimmunoassayRat Serumin vivoNoneNoneStimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm
2941
24983871989
p-Glu-HWSYsLRP
Buserelin9FreeEthylamideLinearMixD-Ser(tBu) at 6th position, Pglu=pyr- GlutamateAnalogue of LHRH (Luteinizing hormone-releasing hormone)Stimulates release of LH, FSH and estradiolBlood collected 0-6 hours after peptide injection500 µg/kg11.2 (elimination t1/2 after 10-60 min of i/v injection)Proteases from serum of women with endometriosisRadioimmunoassay, HPLC(Dose i/v injected)Serum of women with endometriosisin vivoNoneNoneSerum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values
2942
24983871989
p-Glu-HWSYsLRP
Buserelin9FreeEthylamideLinearMixD-Ser(tBu) at 6th positionAnalogue of LHRH (Luteinizing hormone-releasing hormone)Stimulates release of LH, FSH and estradiolBlood collected 0-6 hours after peptide injection500 µg/kg50.4 (elimination t1/2 after 60-120 mins of i/v injection)Proteases from serum of women with endometriosisRadioimmunoassay, HPLC(Dose i/v injected)Serum of women with endometriosisin vivoNoneNoneSerum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values
2946
25212081989
CYFQNCPRG
VP (Vasopressin)9FreeAmidationCyclic (C1-C6)LNoneAnti-diuretic hormone secreted by pitutiary glandAnti-diuretic and regulates retention of waterNot mentionedExogenously administered5.4(lower phase)Proteases from Rabbit plasmaRadioimmunoassayRabbit plasmain vivoNoneNoneNot mentioned
2947
25212081989
CYFQNCPRG
VP (Vasopressin)9FreeAmidationCyclic (C1-C6)LNoneAnti-diuretic hormone secreted by pitutiary glandAnti-diuretic and regulates retention of waterNot mentionedEndogenously administered1.3Proteases from Rabbit plasmaRadioimmunoassayRabbit plasmain vivoNoneNoneNot mentioned
2948
25212081989
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneSyntheticNatriuretic and vasodilatorNot mentionedExogenously administered1.2Proteases from Rabbit plasmaRadioimmunoassayRabbit plasmain vivoNoneNoneNot mentioned
2949
25212081989
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneSyntheticNatriuretic and vasodilatorNot mentionedEndoogenously administered3.2Proteases from Rabbit plasmaRadioimmunoassayRabbit plasmain vivoNoneNoneNot mentioned
2951
28662221985
YADAIFTNSYRKVLGQLSARKLLQDIMSR
hGRF-1(1-29) (Human growth hormone-releasing factor)29FreeAmidationLinearLNoneHuman growth hormone-releasing factor Stimulates growth hormone releaseBlood collected 2-60 minutes after peptide injection10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin,1.9 ±0.2 (alpha half life)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivoNoneNoneNot reported
2952
28662221985
YADAIFTNSYRKVLGQLSARKLLQDIMSR
hGRF-1(1-29) (Human growth hormone-releasing factor)29FreeAmidationLinearLNoneHuman growth hormone-releasing factor Stimulates growth hormone releaseBlood collected 2-60 minutes after peptide injection10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin,10.4 ±0.2 (beta or elimination half life)Rat plasma proteasesRadioimmunoassay(Dose i/v injected)Rat plasmain vivoNoneNoneNot reported
2953
28683811986
AGCKNFFWKTFTSC
Somatostatin14FreeFreeCyclic (C3-C14)LNoneGrowth hormone €“inhibiting hormone (GHIH)Inhibitor of Growth hormone secretionBlood sample collected after 10 minutes in 5 minutes interval, followed by 30 minutes thricely at 1250 µg peptide infused1.2-3.6Proteases from plasma of healthy HumanRadioimmunoassayHuman plasmain vivoNoneNoneNot reported
2954
28683811986
AGCKNFFWKTFTSC
Somatostatin14FreeFreeCyclic (C3-C14)LNoneGrowth hormone €“inhibiting hormone (GHIH)Inhibitor of Growth hormone secretionBlood sample collected after 10 minutes in 5 minutes interval, followed by 30 minutes thricely at 1250 µg peptide infused1.4-4.1Proteases from plasma of Human patient (cirrhotic subjects)RadioimmunoassayPlasma of Human patient (cirrhotic subjects)in vivoNoneNoneNot reported
2955
31080681987
GPETLCGAELVDALQFVCGDRGFYFNKPTGYGSSSRRAPQTGIVDECCFRSCDLRRLEMYCAPLKPAKSA
IGF-1 (Insulin-like growth factor-I)70FreeFreeLinearLNonePurified from bovine colostrumMediates growth and developmentBlood collected 12hours after peptide injection6 - 10 µg/Kg<15Proteases from chicken plasmaRadioimmunoassay(Dose i/v injected)Chicken plasmain vivoNoneNoneGH concentrations subsequent to TRH injection were significantly depressed45.1 and 48.2% in IGF-l-treated as compared with control chicks; and GRF-stimulated GH secretion was significantly decreased by IGF-I administration in (41.3%)
2957
16648041991
SQDSAFRIQERLRNSKMAHSSSCFGQKIDRIGAVSRLGCDGLRLF
Rat BNP-45 ( Brain natriuretic peptide-45)45FreeFreeCyclic (C23-C39)LNoneIsolated from rat heart and shown to be a circulating form of rat BNPCardiac Natriuretic PeptideBlood samples collected at 0.5-10 minutes post peptide injection2 µg/150ul saline6.95 (t 1/2 beta or 2nd phase t1/2)Proteases from Mice (WKY)plasmaRadioimmunoassay(Dose i/v injected)Mice (WKY) plasmain vivoNoneNoneUrinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.2
2959
16648041991
SLRRSSCFGGRIDRIGAQSGLGCNSFRY
Rat alpha-ANP (Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneAtrial natriuretic peptideNatriuretic and vasodilatorBlood samples collected at 0.5-10 minutes post peptide injection2 µg/150ul saline4.03 (t 1/2 beta or 2nd phase t1/2)Proteases from Mice (WKY)plasmaRadioimmunoassay(Dose i/v injected)Mice (WKY) plasmain vivoNoneNoneUrinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.4
2960
25240341989
GGFMTSEKSQTPLVTL
[Leu5]Enkephalin18FreeFreeLinearLNoneSomatostatinInhibitor of Growth hormone secretionNot mentionedPeptide 0.04 w/v in 154mM KCl33 ±7Proteases from rat rectal proteasesHPLCRat rectal lumenin vitroNoneNoneNot mentioned
2962
25240341989
GGFMTSEKSQTPLVTL
[3H-Lys9]DE-gamma-E18FreeFreeLinearLNoneNeuroleptic peptideNeuroregulatorNot mentioned6 µg or 200uCi1.2 ±0.6Proteases from rat bloodHPLCRat bloodin vivoNoneNoneNot mentioned
2966
25562151989
DRVYIHPFHL
Angiotensin I (AI)10FreeFreeLinearLNoneDerived from angiotensinPrecusor of angiotensin- II (AII)37 °C100 - 2000 ng/ml0.6Fetal calf serum proteasesRadioimmunoassayPrimary endothelial cells + Fetal calf Serum (20%)in vitroNoneNoneNot mentioned
2974
27141451989
HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-1(72-107) (Glucagon-like peptide-1)36FreeAmidationLinearLNoneGlucagon-like peptide-1 derivativeRegulates glycemic index, inhibits gastric acid secretionNot mentioned14.4ng/kg peptide infused from 45 min as priming dose, followed by 100 - 400 ng/kg/h dose for 45 m17.2 ±2Proteases from Human plasmaRadioimmunoassayHuman plasmain vivoNoneNone200pmol/L and 600pmol/L cause 16% and 23% Inhibition of pentagastrin-stimulated acid secretion respectively
2975
27141451989
HDEFERHAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Truncated GLP-1(78-107)31FreeAmidationLinearLNoneGlucagon-like peptide-1 derivativeRegulates glycemic index, inhibits gastric acid secretionNot mentioned4.8 -14.4ng/kg peptide infused from 45 min as priming dose, followed by 12.5 - 50 ng/kg/h dose for11.4 ±2.1Proteases from Human plasmaRadioimmunoassayHuman plasmain vivoNoneNone200pmol/L of peptide causes 36% Inhibition of pentagastrin-stimulated acid secretion respectively
2976
81477811994
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
CGRP(Calcitonin gene related peptide)37FreeFreeLinearLNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxia37 °C for 5-60 minutes60 µL of 1 nmol/L CGRP4.3 ±0.2Proteases from sheep plasmaRadioimmunoassaySheep plasma before nephrectomyin vitroNoneNoneNot reported
2977
81477811994
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
CGRP(Calcitonin gene related peptide)37FreeFreeLinearLNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxia37 °C for 5-60 minutes60 µL of 1 nmol/L CGRP7.6 ±0.8Proteases from sheep plasmaRadioimmunoassaySheep plasma after 2 days nephrectomyin vitroNoneNoneNot reported
2978
81477811994
ACDTATCVTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
CGRP(Calcitonin gene related peptide)37FreeFreeLinearLNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxia37 °C for 5-60 minutes60 µL of 1 nmol/L CGRP7.3 ±0.4Proteases from sheep plasmaRadioimmunoassaySheep plasma after 5 days nephrectomyin vitroNoneNoneNot reported
2979
82172161993
SDKP
AcSDKP (Acetyl-SDKP)4AcetylationFreeLinearLNoneIsolated from fetal calf bone marrowNatural hemoregulatory37 °C for 24 hours4 X lO-7M, 10 µCi0.75Proteases from Human serumHPLCHuman serumin vitroNoneNoneNot reported
2982
82172161993
SDKP
AcSDKP (Acetyl-SDKP)4AcetylationFreeLinearLNoneIsolated from fetal calf bone marrowNatural hemoregulatory37 °C for 24 hours4 X lO-7M, 10 µCi0.5Proteases from Horse serumHPLCHorse serumin vitroNoneNoneNot reported
2993
82184821993
YRGDS
YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer)5FreeFreeLinearLPeptide covalently attached to Isocyanate containing polyurethane prepolymerSynthetic RGD containing peptideCell attachment propertyNot mentionedNot mentioned0.5 (Half life of 1st phase)Proteases from mouse boodHPLCMouse bloodin vivoNoneNoneNot reported
3000
85452411995
YGGFLRRIRPK
Dynorphin A(1-11)-NH2 analogue 1 (DYN A analogue)11FreeAmidationLinearLNoneHuman placenta Dynorphin A derivativeIncorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.37 °C100 µM42Proteases from mouse brain tissuesHPLCMouse brain homogenatein vitroNoneNoneNot reported
3002
85452411995
YGGFLRRIRPK
Dynorphin A(1-11)-NH2 analogue 3 (DYN A analogue)11FreeAmidationLinearLNoneHuman placenta Dynorphin A derivativeIncorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates.37 °C100 µM43Proteases from mouse brain tissuesHPLCMouse brain homogenatein vitroNoneNoneNot reported
3011
92343361994
HSDAVFTDNYTRLRKQMAVKKYLNSILN
131I-VIP (Vasoactive intestinal peptide)28FreeAmidationLinearLIodinated at TyrNeuropeptideAnti-inflammatory neuropeptideOrgans are collected at 2-60 minutes after administration of drug (by killing organism)250 µg (6MBq in 0.2mL)2.3 ±0.8 (elimination half life)Proteases from rat lung tissuesHPLC(Dose i/v injected)Rat lung tissuesin vivoNoneNoneNot reported
3012
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat adrenomedullin (AM)50FreeAmidationCyclic (C14-C19)LNoneMember of the calcitonin family of peptidesHypotensive effectBlood sample collected after 0.5-20 minutes after drug administration1.0nmol/Kg1.05 ±0.04 (1st phase elimination life)Proteases from SHR rat plasmaRadioimmunoassayRat(SHR) plasmain vivoNoneNoneMean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively
3013
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat adrenomedullin (AM)50FreeAmidationCyclic (C14-C19)LNoneMember of the calcitonin family of peptidesHypotensive effectBlood sample collected after 0.5-20 minutes after drug administration1.0nmol/Kg1.19 ±0.09 (1st phase elimination life)Proteases from WKY rat plasmaRadioimmunoassayRat(WKY) plasmain vivoNoneNoneMean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively
3014
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat adrenomedullin (AM)50FreeAmidationCyclic (C14-C19)LNoneMember of the calcitonin family of peptidesHypotensive effectBlood sample collected after 0.5-20 minutes after drug administration1.0nmol/Kg18.1 ±1.4 (2nd phase elimination life)Proteases from SHR rat plasmaRadioimmunoassayRat(SHR) plasmain vivoNoneNoneMean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively
3015
85426721995
YRQSMNQGSRSTGCRFGTCTMQKLAHQIYQFTDKDKDGMAPRNKISPQGY
Rat adrenomedullin (AM)50FreeAmidationCyclic (C14-C19)LNoneMember of the calcitonin family of peptidesHypotensive effectBlood sample collected after 0.5-20 minutes after drug administration1.0nmol/Kg16.3 ±1.2 (2nd phase elimination life)Proteases from WKY rat plasmaRadioimmunoassayRat(WKY) plasmain vivoNoneNoneMean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively
3016
83952301993
RPPGFSPFR
Bradykinin9FreeFreeLinearLNoneEndogenous peptide of kinin familyVasodilator, Inflammatory mediator37 °C for 15-60 minutes10 µg/L of peptide29 ±1Neutral endopeptides in Human umbilical vein endothelial cellsRadioimmunoassayHuman umbilical vein endithelial cellsin vitroNoneNoneNot reported
3018
83952301993
RPPGFSPFR
Bradykinin9FreeFreeLinearLNoneEndogenous peptide of kinin familyVasodilator, Inflammatory mediator37 °C for 15-60 minutes10 µg/L of peptide46 ±2Neutral endopeptides in Human umbilical vein endothelial cellsRadioimmunoassayHuman umbilical vein endithelial cells+ phosphoramidonin vitroNoneNoneNot reported
3022
83884031993
RRSSCFGGRIDIIGAQSGLGCNSFRY
ile 12-ANP (Atrial natriuretic peptide)26FreeFreeCyclic (C5-C21)LNoneInfusions of atrial natriuretic peptideNatriuretic and vasodilatorBlood sample collected after 15-240 minutes after peptide administration1.5pmol/Kg/min dose of peptide4.1 ±0.4Proteases from Human plasmaRadioimmunoassayHuman plasma(elder men)in vivoNoneNoneIt increases the cGMP approx 3 fold
3025
29455601986
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
hANP (Human Atrial Natriuretic Peptide)28FreeAmidationCyclic (C7-C23)LNoneHormone secreted by heart muscle cellsNatriuretic and vasodilatorNot mentioned98.3 ± 44.6pg/ml5.65Proteases from Human plasmaRadioimmunoassayHuman plasma(bolus injection)in vivoNoneNoneNot reported
3027
184243662008
HAEGTFTSDVSSYLEGQAAKEFIAWLVK
GLP(7-34) (Glucagon like peptide)28AcetylationAmidationLinearLNoneGLP-1 (Glucagon like peptide-1) analogueAntihyperglycemic or incretin effect (Stimulate Insulin release in glucose dependent manner)37C for 2 hours200 µg/ml~34DPP IVMALDI-TOF-MSPeptide in 0.01 M Na2HPO4 bufferin vitroNoneNoneIn the DPP-IV-free rat pancreatic beta cell line RINm5F GLP-1-(7-34)-amide elevated cAMP production with an EC50 of about 40 nM
3028
19112171991
SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF
CGRP (Calcitonin gene-related peptide)37FreeAmidationCyclic (C2-C7)LNoneAlernative spliced product of calcitonon produced by thyroid glandVasodilator and cause tumor hypoxiaNot mentioned300-600pmol9.00 (plasma half-life)Proteases from Human plasmaNot mentionedHuman Plasmain vivoNoneNoneNot reported
3030
29915171985
(Cbc)KFAP
Compound 16 (Ketomethylene pentapeptide analogue)4Cbc=Cyclobutanecarboxylic acidFreeLinearLProline ring is tritiatedPentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitorAngiotensin converting enzyme (ACE) inhibitor and anti-hypertensiveNot mentioned2mg24.4Proteases from rat bloodLiquid scintillation spectrometer(Dose i/v injected) Rat bloodin vivoNoneNonePotent ACE-inhibitor with I50 =7.0nM
3031
29915171985
5(S)-benzamido-4-oxo-6-phenylhexanoyl-P
Compound 1 (Ketomethylene pentapeptide analogue)15(S)-benzamido-4-oxo-6-phenylhexanoylFreeLinearLProline ring is tritiatedPentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitorAngiotensin converting enzyme (ACE) inhibitor and anti-hypertensiveNot mentioned2mg11.6Proteases from rat bloodLiquid scintillation spectrometer(Dose i/v injected) Rat bloodin vivoNoneNonePotent ACE-inhibitor with I50 =70nM
3032
161976092005
PGDSTRKCMDLKGNK
PCK3145 (Prostate secretory protein 94 derived peptide)15FreeFreeLinearLNoneProstate secretory protein 94 (PSP94) derivativeAnti cancerNot mentioned5-80mg/m2Mean Elimination half life: 0.35-1.45 (Mean Elimination half life)Proteases from Human plasmaNot mentionedHuman plamsain vivohttp://www.drugbank.ca/drugs/DB04985NoneNot reported
3034
201584872010
DRDYMGWMDF
PEG10kDa-[(123)I]-CCK-1010FreeAmidationLinearLSO3H Group at Tyr-4, Coupled to PEG(10KDa), PEG=Polyethylene glycol, CCK-10=CholecystokininPeptide Hormone produced by small intestineStimulates the digestion of fat and proteinNot mentionedNot available15Rat blood proteasesHPLCRat bloodin vivoNoneNoneNot reported
3037
202216502010
NHHGRRRRRRRRRRR
R1(NH2GR11) (An arginine-rich cell permeable peptide)15Cu-DOTA (DOTA=1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid)FreeLinearLCu-labelledDerived from prostate cancer cell lines, an arginine-rich cell permeable peptideCell permeable peptideNot mentionedNot available10.7Proteases from mouse bloodFluorescence ImagingMouse bloodin vivoNoneNoneIn PC3, LNCaP, PZ-HPV-7, DU145 and DU145, FITC-NHGR11 displayed much higher uptake efficiency
3038
202216502010
NHHGRRRRRRRRRRR
R1(NH2GR11) (An arginine-rich cell permeable peptide)15Cu-DOTA (DOTA=1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid)FreeLinearLCu-labelledDerived from prostate cancer cell lines, an arginine-rich cell permeable peptideCell permeable peptideNot mentionedNot available17.2 (Elimination half life)Proteases from mouse bloodFluorescence ImagingMouse bloodin vivoNoneNoneIn PC3, LNCaP, PZ-HPV-7, DU145 and DU145, FITC-NHGR11 displayed much higher uptake efficiency
3039
26248871989
pyr-Glu-LTFTPNW
CC-2 (Corpora cardiaca)8FreeAmidationLinearLpyr-Glu= Pyro-Glutamic acidHypertrehalosaemic hormone in cockroachesActivate fat body glycogen phosphorylase and increase haemolymph trehalose2 hours1-2pmol13.2Proteases from Haemolymph of american cockroachNot mentionedHaemolymph of american cockroachin vivoNoneNoneIncrease in carbohydrates in haemolymph; simulates activation of glycogen phosphorylase and induction of trehalose synthesis
3040
14906681992
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
rhGH(Recombinant DNA derived human growth hormone)191FreeFreeLinearLNoneRecombinant DNA derived human growth hormonePromotes growth and developmentNot mentioned4 IU rhGH/m2 BSA18Proteases from Human serumRadioimmunoassay(Intravenous route of injection) human serumin vivoNoneNoneIn a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight.
3041
14906681992
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
rhGH(Recombinant DNA derived human growth hormone)191FreeFreeLinearLNoneRecombinant DNA derived human growth hormonePromotes growth and developmentNot mentioned4 IU rhGH/m2 BSA2.59 ±1.32Proteases from Human serumRadioimmunoassay(Subcutaneous route of injection) human serumin vivoNoneNoneIn a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight.
3042
14906681992
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
rhGH(Recombinant DNA derived human growth hormone)191FreeFreeLinearLNoneRecombinant DNA derived human growth hormonePromotes growth and developmentNot mentioned10 IU rhGH/m2 BSA4.29 ±1.89Proteases from Human serumRadioimmunoassay(Subcutaneous route of injection) human serumin vivoNoneNoneIn a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight.
3043
14906681992
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
rhGH(Recombinant DNA derived human growth hormone)191FreeFreeLinearLNoneRecombinant DNA derived human growth hormonePromotes growth and developmentNot mentioned4 IU rhGH/m2 BSA6.06 ±2.64Proteases from Human serumRadioimmunoassay(Intramuscular route of injection)human serumin vivoNoneNoneIn a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight.
3044
63612341983
Pyr-QRLGNQWAVGHLM
Amphibian bombesin14FreeAmidationLinearLPyr=Pyro-glutamineSkin of the frog Bombina bombinaInsulinotropic agentNot reported5 pmol/kg . min for 30 min and a volume of 1 ml/min.3Calf blood proteasesRadioimmunoassayArterial blood sample of pedigree jersey calvesin vivo18185064NoneNot mentioned
3045
63612341983
VPLPAGGGTVLTKMYPRGNHWAVGHLM
Porcine gastrin releasing peptide27FreeAmidationLinearLNoneGastrin releasing peptideStimulates the release of GastrinNot reported5 pmol/kg . min for 30 min and a volume of 1 ml/min.3Calf blood proteasesRadioimmunoassayArterial blood sample of pedigree jersey calvesin vivo18185064NoneNot mentioned
3047
103774271999
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP ( Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneCardiac atriacardiovascular homeostasisBlood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide0.2 µci/mouse of [125I]ANP1.44 ±0.05Npr3+/+ mice blood proteasesRadioimmunoassayNpr3+/+ mice blood samplein vivo6230082NoneBlood pressure=118.7 ±1.9 mmHg
3048
103774272000
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
ANP ( Atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneCardiac atriacardiovascular homeostasisBlood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide0.2 µci/mouse of [125I]ANP2.4 ±0.08Npr3-/- mice blood proteasesRadioimmunoassayNpr3-/- mice blood samplein vivo6230082NoneBlood pressure=110.4 ±2.3 mmHg
3049
29393121986
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
α-hANP (Alpha human atrial natriuretic peptide)28FreeFreeCyclic (C7-C23)LNoneHuman atrial extractsNatriuretic and hypotensive actionsVenous samples were drawn at 1 mln intervals for 10 mlns after injectlon and then at 15 and 30 mlns.100 µg2.5Human blood proteasesRadioimmunoassayIntravenous bolus injection of 100μg alpha human atrial natriuretic factor in humanin vivoNoneNoneNot mentioned
3075
120839772002
PHWSYlLRP
Leuprorelin95-oxoEthylacetateLinearMixNoneSynthetic agonist analogue of gonadotropin-releasing hormoneSuppression of gonadal steroid synthesis, resulting in pharmacological castrationNot mentioned100μg/kg8.4 ±4(t1/2α)Diestrous female rats blood proteasesRadioimmunoassayIntravenous injection in diestrous female ratsin vivoNoneNoneNot mentioned
3076
120839772002
PHWSYlLRP
Leuprorelin95-oxoEthylacetateLinearMixNoneSynthetic agonist analogue of gonadotropin-releasing hormoneSuppression of gonadal steroid synthesis, resulting in pharmacological castrationNot mentioned100μg/kg33.2 ±6.8(t1/2β)Diestrous female rats blood proteasesRadioimmunoassayIntravenous injection in diestrous female ratsin vivoNoneNoneNot mentioned
3079
120839772002
PHWSYlLRP
Leuprorelin95-oxoEthylacetateLinearMixNoneSynthetic agonist analogue of gonadotropin-releasing hormoneSuppression of gonadal steroid synthesis, resulting in pharmacological castrationNot mentioned10 µg32(t1/2β)Pregnant female rats blood proteasesRadioimmunoassaySubcutaneous injection in pregnant ratsin vivo3083092NoneNot mentioned
3080
120839772002
pGlu-HWSYGLRPG
GnRH (Gonadotropin-releasing hormone)10PyroGlu=Pyroglutamic acidFreeLinearLpGlu=pyroglutamic acidHypothalamic neuronsRegulating the synthesis and secretion of the gonadotropins luteinising hormone (LH) and follicle-stimulating hormone (FSH).Not mentionedNot mentionedless than 15Human plasma proteasesRadioimmunoassayHuman bloodin vivoNoneNoneNot mentioned
3081
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned2.17 ±0.05Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographyBreast fed healthy infants(0-1years)serum samplein vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3082
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned2.48 ±0.007Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographyFormula fed healthy infants(0-1years)serum samplein vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3083
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned2.26 ±0.06Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographySerum sample of healthy infant boys(0-1 years)in vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3084
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned2.51 ±0.08Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographySerum sample of healthy infant girls(0-1 years)in vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3085
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned2.37 ±0.05Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographySerum sample of children(0-1 years)in vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3086
154525962004
YGGFL
Leu-enkephalin5FreeFreeLinearLNoneEndogenous opioid ligandIndicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory.Not mentionedNot mentioned3.10 ±0.05Enkephalin-degrading enzymes present in blood serumAccumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatographySerum sample of adultsin vivoO. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, etNoneNot mentioned
3093
190235442008
RKDVY
TP5 (Thymopentin)5FreeFreeLinearLNoneSynthetic peptide of thymic hormoneImmunomodulatorNot mentionedNot mentioned5.6 ±0.7Rabbit plasma proteasesHPLCheparinized rabbit plasmain vitrohttp://www.drugbank.ca/drugs/DB00112NoneIL2 concentration in mouse serum:0.65pg/ml,macrophage clearance index(K value)=0.0132 ±0.0008,phagocytic index(α value=3.43 ±0.29.
3094
203826952010
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
hGLP-1[7-36] (Human glucagon like peptide-1)30FreeAmidationLinearLNoneIncretin released by intestinal L cellsMetabolism regulation1 hour40 nm(1μg/μl upto 500μl)50Rat blood proteasesHPLCRat blood plasmain vitrohttp://www.drugbank.ca/drugs/DB00113NonecAMP stimulation,EC50=0.08nM
3119
210367182010
QWAVGHLM
177Lu-AMBA9177Lu,DO3A-CH2CO-G-(4-aminobenzoyl)AmidationLinearLNoneSynthetic Bombesin like peptideClinical trials for use as systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients.Not mentioned10μg/mouse0.52 ±0.05(t1/2α)Mice plasma proteasesRadio-HPLCIntravenous injection in PC-3M-luc-C6 tumour-bearing micein vivohttp://www.drugbank.ca/drugs/DB00138NoneIn vitro stability =24.3 ±21.9% after 48 hours
3123
219861002011
YaGFlC
DALCE [(D-Ala2, Leu5, Cys6)-enkephalin]6FreeFreeLinearMixNoneEnkephalin derativeTreatment of ischemiaNot mentioned1mg/Kg9.1 ±2.4Rats plasma proteasesLC-MSIntravenous injection in male Sprague €“Dawley ratsin vivohttp://www.drugbank.ca/drugs/DB00142NoneNot mentioned
3124
219861002011
YaGFl
DADLE [(D-Ala2, Leu5)-enkephalin]5FreeFreeLinearMixNoneOpoid peptideNeuromodulatorNot mentioned1mg/Kg(200-250μl)4.6Rats plasma proteasesHPLC with tandem LC/MS/MSRat plasmain vivohttp://www.drugbank.ca/drugs/DB00143NoneNot mentioned
3125
219861002011
YaGFlC
CMD-Cys-DALCE6FreeThiolated carboxymethyl dextran(CMD) cysteine conjugated via disulfide bondLinearMixNoneEnkephalin derativeTreatment of ischemiaNot mentioned4.5 mg/kg corresponding to 1 mg/kg of DALCE56 ±6.0Rats plasma proteasesLC-MSIntravenous injection in male Sprague €“Dawley ratsin vivohttp://www.drugbank.ca/drugs/DB00144NoneNot mentioned
3126
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
HR2 (wild type) [HR2 regions of the HIV-1 envelope glycoprotein gp41]41FreeFreeLinearLNoneHR2 regions of the HIV-1 envelope glycoprotein gp41Inhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM37.2Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00145NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=1.5 ± 0.1nM
3127
227705642012
CEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLW
N-terminus of HR242FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.6Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00146NoneNot mentioned
3128
227705642012
CEWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLW
N-terminus-PEG750 of HR242Pegylation-PEG750FreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM40Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00147NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=7.2 ± 0.7nM
3130
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
R4C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM37.4Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00149NoneNot mentioned
3131
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
R4C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 4th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM44.1Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00150NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.1 ± 1.1nM
3133
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
S11C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.9Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00152NoneNot mentioned
3134
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
S11C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 11th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM50.2Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00153NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.4 ± 0.8nM
3136
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
S15C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM39.9Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00155NoneNot mentioned
3137
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
S15C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 15th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM53.7Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00156NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.1 ± 1.0nM
3139
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
E18C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.4Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00158NoneNot mentioned
3140
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
E18C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 18th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM50.3Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00159NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.5 ± 1.0nM
3142
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
N22C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.9Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00161NoneNot mentioned
3143
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
N22C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 22nd positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM51.8Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00162NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.2 ± 0.9nM
3145
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
Q29C derivative of HR241FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.6Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00164NoneNot mentioned
3146
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNECELLELDKWASLW
Q29C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 29th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM58.1Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00165NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.2 ± 0.8nM
3148
227705642012
EWDREINNYTSLIHSLIEESQNQQEKNEQELLELDKWASLWC
C terminus derivative of HR242FreeFreeLinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM39Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00167NoneNot mentioned
3151
227705642012
EWDREINNYTSLIHSLIEECQNQQEKNEQELLELDKWASLW
S20C derivative of HR241FreePegylation (PEG2000)LinearLNoneModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM38.6Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00170NoneNot mentioned
3152
227705642012
EWDREINNYTSLIHSLIEECQNQQEKNEQELLELDKWASLW
S20C-PEG750 derivative of HR241FreeFreeLinearLPegylation-PEG750 of cysteine at 20th positionModified HR2 wild type peptideInhibitor to prevent virus ˆ’host cell membrane fusionNot mentioned20μM42Bovine TrypsinTrypsin degradation assay, Analytical reverse phase HPLCSolutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4)in vitrohttp://www.drugbank.ca/drugs/DB00171NoneCell ˆ’Cell Fusion Inhibition Efficacy (IC50)>400
3154
230994312012
HwAWfK
GHRP-6 (Growth Hormone-Releasing Peptide-6)6FreeAmidationLinearMixNoneSynthetic molecule structurally related to Met-enkephalinCytoprotective,antioxidant in natureNot mentioned100 μg/kg of the body weight0.14 ±0.03(t1/2α)human plasma proteasesLC-MSIntravenous bolus administartion in 9 healthy male subjectsin vivohttp://www.drugbank.ca/drugs/DB00173NoneNot mentioned
3156
230994312012
HwAWfK
GHRP-6 (Growth Hormone-Releasing Peptide-6)8FreeAmidationLinearMixNoneSynthetic molecule structurally related to Met-enkephalinCytoprotective,antioxidant in natureNot mentioned200 μg/kg of the body weight0.15 ±0.06(t1/2α)human plasma proteasesLC-MSIntravenous bolus administartion in 9 healthy male subjectsin vivohttp://www.drugbank.ca/drugs/DB00175NoneNot mentioned
3158
230994312012
HwAWfK
GHRP-6 (Growth Hormone-Releasing Peptide-6)10FreeAmidationLinearMixNoneSynthetic molecule structurally related to Met-enkephalinCytoprotective,antioxidant in natureNot mentioned400 μg/kg of the body weight0.09 ±0.01(t1/2α)human plasma proteasesLC-MSIntravenous bolus administartion in 9 healthy male subjectsin vivohttp://www.drugbank.ca/drugs/DB00177NoneNot mentioned
3160
231968062012
YGRKKRRQRRR
TAMRA-TAT [5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT]115-(and-6)-carboxytetramethylrhodamine(TAMRA)FreeLinearLNoneHIVCell penetrating peptideNot mentioned60 μg/g6.7Modified simulated intestinal fluid with pancreatic enzymesHPLC with fluorescence detectionModified simulated intestinal fluidin vitrohttp://www.drugbank.ca/drugs/DB00179NoneFluorescence intensity (intestinal delivery)=4.0×105 in Duodenum, 6.0×105 in Jejunum, 4.0×105 in Ileum, 1×105 in Colon
3161
231968062012
YGRKKRRQRRR
TAMRA-TAT microemulsion115-(and-6)-carboxytetramethylrhodamine(TAMRA)FreeLinearLNoneHIVCell penetrating peptideNot mentionedMicroemulsion composition: Miglyol 812/Capmul MCM/Tween 80/TAMRA-TAT solution at the weight ratio of19.4Modified simulated intestinal fluid with pancreatic enzymesHPLC with fluorescence detectionModified simulated intestinal fluidin vitrohttp://www.drugbank.ca/drugs/DB00180NoneFluorescence I ntensity (intestinal delivery)< 1.0×105 in Duodenum, Jejunum, Ileum, Colon
3167
12136601975
FVNQHLCGSHLVEALYLVCGERGFFYTPKARREAQNPQAGAVELGGGLGGLNALALEGPPQKRGIVEQCCTSICSLYQLENYCN
Procine Proinsulin84FreeFreeCyclic (C7-C70,C19-C83,C69-C74)LNoneProinsulinNot mentionedNot reported5-8.6 µg/kg were injected.8.2 ±0.3Porcine blood proteasesRadioimmunoassayPorcine bloodin vivohttp://www.drugbank.ca/drugs/DB00186NoneNot reported
3168
12136601975
RREAQNPQAGAVELGGGLGGLNALALEGPPQKRG
Procine C-Peptide34FreeFreeLinearLNoneProinsulinNot mentionedNot reported5-8.6 µg/kg were injected.9.9 ±0.5Porcine blood proteasesRadioimmunoassayPorcine bloodin vivohttp://www.drugbank.ca/drugs/DB00187NoneNot reported
3169
77878271994
SSSHPIFHRGEFSVCDSVSVWVGDKTTATDIKGKEVMVLGEVNINNSVFKQYFFETKCRDPNPVDSGCRGIDSKHWNSYCTTTHTFVKALTMDGKQAAWRFIRIDTACVCVLSRKAVRRA
125I-β-NGF120FreeFreeCyclic (3 disulphide bonds between C15-C80, C58-C108, C68-C110)LNoneβ-nerve growth factorNerve growth promoting peptideBlood samples (250 µl) were obtained from the catheterized carotid artery 15, 30, 45 and 60 min afte800 000 cpm of 125I-7S-NGF or 125I-β-NGF (diluted in 200 µl of saline)36.3 + 2.20Rats blood proteasesColumn chromatographyIntravenouly injected in adult male Wistar ratsin vivohttp://www.drugbank.ca/drugs/DB00188NoneNot reported
3170
79623021994
YADAIFTNSYRKVLGQLSARKLLQDIMSR
GHRH29FreeAmidationLinearLNoneSyntheticGrowth hormone-releasing hormone (GHRH) stimulates growth hormone (GH) gene transcription, synthesis, and secretion of growth hormone via growth hormone-releasing hormone receptor (GHRH-R)Blood samples were obtained at 5 min intervals for measurement of serum GH concentrations and at theIntravenous dose of 1 µg/kg followed by a 15 min infusion of saline in human subjects.18.5 ±0.8Human blood proteasesImmunoradiometric assay (IRMA)Human bloodin vivohttp://www.drugbank.ca/drugs/DB00189NoneNot reported
3171
78992301994
YGGFL
Leucine enkephalin5FreeFreeLinearLNoneLeucine enkephalinOpioid peptideNot reported0.63 mg/ml40Sheep nasal wash fluid proteasesHPLCSheep nasal wash fluidin vitrohttp://www.drugbank.ca/drugs/DB00190NoneNot reported
3172
78992301994
YGGFL
Leucine enkephalin5FreeFreeLinearLNoneLeucine enkephalinOpioid peptideNot reported20 µg/ml12Sheep nasal mucosal proteasesHPLCSheep nasal mucosal tissue homogenatein vitrohttp://www.drugbank.ca/drugs/DB00191NoneNot reported
3173
78992301994
GGFL
des-tyrosine leucine enkephalin4FreeFreeLinearLNonedes-tyrosine leucine enkephalinOpioid peptideNot reported0.63 mg/ml13Sheep nasal wash fluid proteasesHPLCSheep nasal wash fluidin vitrohttp://www.drugbank.ca/drugs/DB00192NoneNot reported
3174
78992301994
GGFL
des-tyrosine leucine enkephalin4FreeFreeLinearLNonedes-tyrosine leucine enkephalinOpioid peptideNot reported20 µg/ml7Sheep nasal mucosal proteasesHPLCSheep nasal mucosal tissue homogenatein vitrohttp://www.drugbank.ca/drugs/DB00193NoneNot reported
3175
81008401993
AGCKNFFWKTFTSC
Somatostatin (SOM)14FreeFreeCyclic (C3-C14)LNoneSyntheticGrowth hormone inhibiting hormone (GHIH)Not reportedNot reported<5Rats blood proteasesNot mentionedRats plasmain vivohttp://www.drugbank.ca/drugs/DB00194NoneNot reported
3176
81008401993
YPSKPDNPGEDAPAEDLARYYSALRHYINLITRQRY
Neuropeptide Y36FreeAmidationLinearLNoneNeuropeptideStimulation of the right cardiac sympathetic nerveNot reportedNot reported21Dogs blood proteasesNot mentionedDogs plasmain vivohttp://www.drugbank.ca/drugs/DB00195NoneNot reported
3177
80827051994
EAKSQGGSN
Facteur thymique serique (FTS)9FreeFreeLinearLNoneThymic peptide hormoneSuppressed hyperglycemiaNot reportedNot reported2 to 3Rats blood proteasesRadioimmunoassayIntravenouly injected in male Wistar ratsin vivohttp://www.drugbank.ca/drugs/DB00196NonePlasma glucose in FTS-treated group=15.7 ± 1.8 (mmol/l)while in control Plasma glucose=28.3 ±2.1 ( µmol/l)
3178
80356441994
YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
Adrenomedullin (ADM)52FreeFreeLinearLNoneSyntheticHormone in circulation controlNot reportedIntraarterial doses of 0.01-0.3 nmol55 to 80Cat blood proteasesHPLCHind limb vascular bed of the catin vivohttp://www.drugbank.ca/drugs/DB00197NoneNot reported
3179
80356441994
GCRFGTCT
ADM 15-228FreeFreeLinearLNoneCarboxy terminal 15-52 fragment of adrenomedullinAn inhibitor of the cellular actions of adrenomedullinNot reportedIntraarterial doses of 0.01-0.3 nmol55 to 80Cat blood proteasesHPLCHind limb vascular bed of the catin vivohttp://www.drugbank.ca/drugs/DB00198NoneNot reported
3181
172045512007
FNAPFDVGIKLSGAQYQQHGRAL
Rat Obestatin23FreeAmidationLinearLNoneProghrelin frpm humanEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion0 - 60 minutes10 μg22 ±2Protease from rat plasmaRadioimmunoassayIntravenous injection of peptide into Sprague Dawley ratsin vivoNoneNoneCo-administration of obestatin with ghrelin inhibited food intake.
3182
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg19Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mousein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3183
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg53Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + P8340 protease inhibitor cocktailin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3184
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg39Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + EDTAin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3185
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg20.5Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + Soybean trypsin inhibitorin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3186
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg20.5Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + APMSFin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3187
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg24Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + 1,10-Phenanthrolinin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3188
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg20Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + Captoprilin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3189
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg17Proteases from Crude brain homogenate of mouseHPLCCrude brain homogenate of mouse + Chymostatinin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3190
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg27Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenatein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3193
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg38.5Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenate + Soybean trypsin inhibitorin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3194
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg16Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenate+ APMSFin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3195
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg28Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenate + 1,10-Phenanthrolinin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3196
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg28Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenate + Captoprilin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3197
194228572009
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 120 minutes90 μg29.5Proteases from Membrane brain HomogenateHPLCMembrane brain Homogenate+ Chymostatinin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNo suppressive effects of obestatin on food or water intake were observed
3198
186021972008
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.490 μg42.2 [40.5, 44.0]Proteases from mouse plasmaHPLC, LC-UV/MSMouse plasmain vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3199
186021972008
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.590 μg12.6 [11.4, 14.1]Proteases from Mouse liver homogenateHPLC, LC-UV/MSMouse liver homogenatein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3200
186021972008
FNAPFDVGIKLSGAQYQQHGRAL
Mouse Obestatin23FreeAmidationLinearLNoneProghrelin from mouseEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.690 μg30.0 [27.8, 32.6]Proteases from Mouse stomach homogenateHPLC, LC-UV/MSMouse stomach homogenatein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3204
186021972008
FNAPFDVGIKLSGVQYQQHSQAL
Human Obestatin23FreeAmidationLinearLNoneProghrelin frpm humanEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.1090 μg13.3 [12.7, 14.0]Proteases from mouse liver homogenateHPLC, LC-UV/MSMouse liver homogenatein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3205
186021972008
FNAPFDVGIKLSGVQYQQHSQAL
Human Obestatin23FreeAmidationLinearLNoneProghrelin frpm humanEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.1190 μg28.0 [25.8, 30.5]Proteases from mouse liver homogenate+protease inhibitor cocktaiHPLC, LC-UV/MSMouse liver homogenate with protease inhibitor cocktailin vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3207
186021972008
FNAPFDVGIKLSGVQYQQHSQAL
Mono-iodinated human obestatin23FreeAmidationLinearLIodination at tyr16Proghrelin frpm humanEnergy balance, Inhibit Ghrelin-induced Growth Hormone secretion37 °C for 0 - 60 minutes, pH 7.1290 μg15.1 [9.1, 45.0]Proteases from Mouse liver homogenateHPLC, LC-UV/MSMouse liver homogenatein vitrohttp://www.sigmaaldrich.com/catalog/product/sigma/NoneNot reported
3208
83532801993
ASISGRDTHRLTRTLNCSSIVKEIIGKLPEPELKTDDEGPSLRNKSFRRVNLSKFVESQGEVDPEDRYVIKSNLQKLNCCLPTSANDSALPGVFIRDLDDFRKKLRFYMVHLNDLETVLTSRPPQPASGSVSPNRGTVEC
Interleukin-3 (IL-3)140FreeFreeCyclic (C17-C80,C79-C140)LGlycosylation at 84thand 112th positionIL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophilsHematopoietic growth factorNot mentioned1,000 biologic units2.1 (α half life)Balb/c mice blood proteasesELISAInjected intravenously in Balb/c mice bloodin vivohttp://www.uniprot.org/uniprot/P01586NoneMice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field
3209
83532801993
ASISGRDTHRLTRTLNCSSIVKEIIGKLPEPELKTDDEGPSLRNKSFRRVNLSKFVESQGEVDPEDRYVIKSNLQKLNCCLPTSANDSALPGVFIRDLDDFRKKLRFYMVHLNDLETVLTSRPPQPASGSVSPNRGTVEC
Interleukin-3 (IL-3)140FreeFreeCyclic (C17-C80,C79-C140)LGlycosylation at 84thand 112th positionIL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophilsHematopoietic growth factorNot mentioned1,000 biologic units10.0 (β half life)Balb/c mice blood proteasesELISAInjected intravenously in Balb/c mice bloodin vivohttp://www.uniprot.org/uniprot/P01586NoneMice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field
3210
83532801993
ASISGRDTHRLTRTLNCSSIVKEIIGKLPEPELKTDDEGPSLRNKSFRRVNLSKFVESQGEVDPEDRYVIKSNLQKLNCCLPTSANDSALPGVFIRDLDDFRKKLRFYMVHLNDLETVLTSRPPQPASGSVSPNRGTVEC
Interleukin-3 (IL-3)140FreeFreeCyclic (C17-C80,C79-C140)LGlycosylation at 84thand 112th positionIL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophilsHematopoietic growth factorNot mentioned1,000 biologic units3.6 (α half-life)Balb/c mice blood proteasesELISAInjected intravenously in Balb/c mice bloodin vivohttp://www.uniprot.org/uniprot/P01586NoneMice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field
3211
83532801993
ASISGRDTHRLTRTLNCSSIVKEIIGKLPEPELKTDDEGPSLRNKSFRRVNLSKFVESQGEVDPEDRYVIKSNLQKLNCCLPTSANDSALPGVFIRDLDDFRKKLRFYMVHLNDLETVLTSRPPQPASGSVSPNRGTVEC
Interleukin-3 (IL-3)140FreeFreeCyclic (C17-C80,C79-C140)LGlycosylation at 84thand 112th positionIL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophilsHematopoietic growth factorNot mentioned1,000 biologic units30.8 (β half life)Balb/c mice blood proteasesELISAInjected intravenously in Balb/c mice bloodin vivohttp://www.uniprot.org/uniprot/P01586NoneMice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field
3212
191153922009
HPAGKRPCKMQAFRIWDTNQKTFYLRNNQLIAGYLQGPNTKLEEKIDMVPIDFRNVFLGIHGGKLCLSCVKSGDDTKLQLEEVNITDLNKNKEEDKRFTFIRSETGPTTSFESLACPGWFLCTTLEADHPVSLTNTPKEPCTVTKFYFQEDQ
Interleukin-1 Receptor Antagonist (IL-1ra)152FreeFreeCyclic(66-116)LGlycosylation at 84th positionInterleukin-1 Receptor AntagonistThe natural specific receptor antagonist (IL-1ra) binds to IL-1RI but does not initiate signaling as it does not engage the IL1R accessory protein and therefore acts as a receptor antagonist.Not mentionedNot mentioned6 to 15Rats blood proteasesNot mentionedRat bloodin vivohttp://www.uniprot.org/uniprot/P25086NoneSignificant depression of LTP in the group of animals that received intracerebroventricular injection of Aβ-peptide (1 €“40) compared with control animals injected with vehicle.
4006
387890612024
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntidiabetesBlood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr1 mg/kg0.5 ± 0.1Male SD rats plasma proteaseUHPLCMale SD rats plasmaIn VivoPDB id: 7MLLNoneN.A.
4019
387372832024
LAEAKVLANRELDKYGVSDFYKRLINKAKTVEGVEALKLHILAALP-FRRG-(E5C3)-(GN)
ABD035-immunoGNN.A.P1h3His-tagLinearLHumanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-NSynthetic AntitumorBlood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min0.1 μmol/kg35.22BALB/c mice serum proteaseELISABALB/c mice serumIn VivoNoneNoneCytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4020
387372832024
FRRG-(E5C3)-(GN)
immunoGNN.A.P1h3His-tagLinearLHumanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-NSynthetic AntitumorBlood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min0.1 μmol/kg4.599BALB/c mice serum proteaseELISABALB/c mice serumIn VivoNoneNoneCytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4021
387372832024
DIQMTQSPSSLSAVGDRVTITCRASQSISSYLNWYQQKPGKAPKLLIYRNSPLQSGVPSRFSGSGSGTDFTLTISSLQPEDFATYYCQQTYRVPPTFGQGTKVEIKR-FRRG-(E5C3)-(GN)
dAb7h8-immunoGNN.A.P1h3His-tagLinearLHumanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-NSynthetic AntitumorBlood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min0.1 μmol/kg31.25BALB/c mice serum proteaseELISABALB/c mice serumIn VivoNoneNoneCytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation
4031
386139962024
AGILKRW
PepH37FreeAmidationLinearLNoneSyntheticAnticancerAt different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C1 mM21.00 ± 2.91Human serum proteaseRP-HPLCHuman serumIn VitroNoneNoneIC50 > 100.0 for TNBC MDA-MB-231 Monolayer
4041
384936732024
ALWPPNLHAWVP
Peptide ALW12FreeFreeLinearLNoneSyntheticAlleviating Lupus NephritisN.A.12.5 mg/kg0.315 (Elimination Half Life)Cd1 mice plasma proteaseN.A.CD1 mice plasmaIn VivoNoneNoneKD(M) = 1.99*10-4 (Binding affinity of peptides to anti-dsDNA IgG3)
4057
383120522024
KXCRGDCFCX
Maraciclatide (99mTc)7AcetylationFreeCyclic(Ac-Cys8 Bond, Cys2-Cys6 Disulfide Bond)LRadiolabelled with technetium, X= Unknown Structure syntheticNovel Diagnostic Imaging Agent For A Range Of Pathological ConditionsBlood and plasma samples were collected at 10 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, and 7 days post-administrationThe data acquired from all participants who received 99mTc-maraciclatide within the expected clinical range (15, 75 µg, 150) were pooled1 (Terminal Elimination Half Life)Human Plasma ProteaseGamma counterHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/73050806NoneN.A.
4061
381049072024
Y-(d-Dab)-RFFwKTF
[Al18F]NODA-MPAA-HTA8Conjugating 18F nuclide with a modified KE108 peptide, MPAA modification at N terminalThe amino group of KE108 peptide conjugated with the carboxyl group of NODACyclic(d-Dab2-Phe8)MixD-Tryp amino acid substituition, d-Dab = Diaminobutyric acid18F-radiolabeled somatostatin analogueUsed for PET imaging of Neuroendocrine tumors (NETs)Blood samples were collected from the retroorbital plexus into capillary at 5, 10, 15, 30,60 and 120 minN.A.37.63 ± 13.05 (Elimination Half Life)BALB/c mice blood proteaseGamma counterBALB/c mice blood sampleIn VivoNoneNoneAffinity of [Al18F]NODA-MPAA-HTA (Kd = 8.77 ± 1.14 nM, n = 4) 
4079
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing0.1 mg/kg3.49 (Initial Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4080
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing1 mg/kg3.34 (Initial Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4081
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing10 mg/kg7.64 (Initial Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4082
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing0.1 mg/kg18.8 (Terminal Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4083
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing1 mg/kg10 (Terminal Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4084
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing10 mg/kg10.2 (Terminal Elimination Phase)Male wistar rats plasma proteaseLC-MS/MSMale wistar rat plasmaIn VivoNoneEP 2023067975 WN.A.
4085
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg8.4 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma after day 1 repeated doseIn VivoNoneEP 2023067975 WN.A.
4086
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg7.33 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma after day 1 repeated doseIn VivoNoneEP 2023067975 WN.A.
4087
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg7.66 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma after day 14 repeated doseIn VivoNoneEP 2023067975 WN.A.
4088
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg7.11 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma after day 14 repeated doseIn VivoNoneEP 2023067975 WN.A.
4089
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg7 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma after day 1 repeated doseIn VivoNoneEP 2023067975 WN.A.
4090
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg8 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma after day 1 repeated doseIn VivoNoneEP 2023067975 WN.A.
4091
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg6.67 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma after Day 14 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4092
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg6.85 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma After Day 14 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4093
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg7.8 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4094
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg7.16 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4095
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg7.31 (Elimination Half Life)Male wistar rats plasma proteaseLC-MS/MSMale wistar rats plasma After Day 14 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4096
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg7.04 (Elimination Half Life)Female wistar rats plasma proteaseLC-MS/MSFemale wistar rats plasma After Day 14 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4097
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg4.68 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4098
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg4.83 (Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4099
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg6.59 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4100
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 141 mg/kg4.66 (Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4101
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg6.01 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4102
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg5.7(Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4103
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg6.05 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4104
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 143 mg/kg6.13 (Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4105
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg5.09 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4106
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg5.41 (Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4107
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg6 (Elimination Half Life)Male dogs plasma proteaseLC-MS/MSMale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4108
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatorySamples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 1410 mg/kg5.9 (Elimination Half Life)Female dogs plasma proteaseLC-MS/MSFemale dogs plasma After Day 1 Repeated DoseIn VivoNoneEP 2023067975 WN.A.
4111
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start100μg/kg1.15 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasmaIn VivoNoneEP 2023067975 WN.A.
4112
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start150 μg/kg1.15 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasmaIn VivoNoneEP 2023067975 WN.A.
4113
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start50 μg/kg1.38 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasma received three 8 hours apart 30-min peptide 1 repeated dose In VivoNoneEP 2023067975 WN.A.
4114
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start100μg/kg2.18 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasma received three 8 hours apart 30-min peptide 1 repeated dose In VivoNoneEP 2023067975 WN.A.
4115
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start140 μg/kg1.94 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasma received three 8 hours apart 30-min peptide 1 repeated dose In VivoNoneEP 2023067975 WN.A.
4116
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start200 μg/kg1.94 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasma received three 8 hours apart 30-min peptide 1 repeated dose In VivoNoneEP 2023067975 WN.A.
4117
N.A.2024
AMVSEFLKQAWFIENEEQEYVQTLKSSKGGPGSAVSPYPTFNPSSDV
Peptide 147FreeAmidationLinearLV24L modificationsAnnexin A1 DerivativeAntiinflammatoryBlood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start250 μg/kg1.88 (Elimination Half Life)Human plasma proteaseLC-MS/MSHuman plasma received three 8 hours apart 30-min peptide 1 repeated dose In VivoNoneEP 2023067975 WN.A.
4118
388636462024
N.A.
(89Zr, Mn)-WPMNsN.A.FreeFreeLinearLMn and 89Zr labeling, MNPs modified with WL12-SH WL12 derivativeTargets PD-L1Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h0.5 mg/ml0.1234 (Fast) (Metabolic Half Life)KM mouse blood proteaseRadioactivity assay using γ-counterKM mouse bloodIn VivoNoneNoneN.A.
4173
380270632023
QVTLKESGPGILQPSQTLSLTCSFSGFSLNTFGMGVSWIRQPSGKGLEWLAHIFWDDDKHYNPSLKSRLTISKDTSNNQVFLKITTVDTADTATYYCVRYGFDGFPYWGQGTGGGGSGGGGSGGGGSDVVMTQTPLSLPVSLGDQASISCRSNQSLVHSNGNTYLHWYLQKPGQSPKLLIYKVSNRFSGVPDRPSGSGSGTDFTLKISRVEAEDLGFYFCSQSTRVPWTFGGGTKLEIKR 
ScFv9304FreeFreeLinearLBiotinylationThe scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ)Treatment of AD and Parkinson diseasePlasma was collected at 0, 2, 4, 8, and 24 h after injection250 μg0.74TgCRND8 mice plasma proteaseDirect ELISATgCRND8 mice plasmaIn VivoNoneNoneN.A.
4176
378803182023
VAIALKAAHYHTHKE
L315FreeAmidationLinearLNoneDerived from calciterminAntimicrobial37 °C0.0001 M20Human plasma proteaseHPLCHuman plasma with 1 ml of ammonium acetate buffer (pH 7.4) In VitroNoneNoneCFU = 189 ± 23 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation)
4177
378803182023
VAIALKAAHYHTHKE
Wild-type Calcitermin (WT)15FreeFreeLinearLNoneC-terminal cleavage fragment of calgranulin CAntimicrobial37 °C0.0001 M18 ± 3Human plasma proteaseHPLCHuman plasma with 1 ml of ammonium acetate buffer (pH 7.4) In VitroNoneNoneCFU = 28 ± 15 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation)
4178
378754812023
N.A.
IL-15-Cy7N.A.FreeFreeLinearLCy7Derived from Interleukin-15AntitumorThe blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h)N.A.0.69Mice blood proteaseFluorescence spectrophotometryMice bloodIn VivoNoneNoneNot mentioned
4189
373974952023
SLAFVDVLN
Peptide9FreeFreeLinearLRemoving an Asp residueIsolated from Merluccius productus fish protein hydrolysateInhibits BACE-1Blood was taken after 0, 5, and 30 min and 2, 6, and 24 h after injectio4 mg/kg0.69Mouse plasma proteaseMass spectrometryMouse plasmaIn VivoNoneNoneKi(µM)= 0.0940 BACE-1 activity with peptide which has reduced activity due to inhibition by peptide
4190
373909792023
H-Aib-DGTFTSELSRLREGARLQRLLQGLLQGLVGK
BI-343433FreeAmidationLinearLLys33 conjuagted with HLE (fatty acid based half life extension group),Substituting Ser with 2-aminoisobutyric acid (Aib) at position 2Lipidated secretin analogSecretin receptor agonist N.A.30 nmol/kg<15Male NMRI mice plasma proteaseMass spectrometryMale NMRI mice plasma (Non fasted)In VivoNoneNoneEC50 =15.5 pM for BI-3434
4196
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerTimepoints of 0, 10, 20, 30, 60, and 120 min2 μM54.6Beagle dogs plasma proteaseTriple Quadrupole Mass spectrometryBeagle dogs plasmaIn VitroNoneNoneNot mentioned
4197
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerTimepoints of 0, 10, 20, 30, 60, and 120 min2 μM52.7Cynomolgus monkeys plasma proteaseTriple Quadrupole Mass spectrometryCynomolgus monkeys plasma In VitroNoneNoneNot mentioned
4198
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerTimepoints of 0, 10, 20, 30, 60, and 120 min2 μM5.68CD-1 mouse plasma proteaseTriple Quadrupole Mass spectrometryCD-1 mouse plasmaIn VitroNoneNoneNot mentioned
4200
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancer120 minutes2 μM2.72Intestinal fluid proteaseTriple Quadrupole Mass spectrometrySimulated Intestinal Fluid (SIF) at pH = 5.5In VitroNoneNoneEnzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4204
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis2 μM (0.5 mg protein/mL of each species pooled together)32.5CD-1 mouse Liver Microsomes proteaseLC-MS/MSCD-1 mouse Liver Microsomes In VitroNoneNoneN.A.
4205
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis2 μM (0.5 mg protein/mL of each species pooled together)27.7SD rats Liver Microsome ProteaseLC-MS/MSSD rats Liver MicrosomeIn VitroNoneNoneN.A.
4206
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis2 μM (0.5 mg protein/mL of each species pooled together)33Beagle dogs Liver Microsome ProteaseLC-MS/MSBeagle dogs Liver MicrosomeIn VitroNoneNoneN.A.
4207
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis2 μM (0.5 mg protein/mL of each species pooled together)21.8Cynomolgus monkeys Liver Microsome ProteaseLC-MS/MSCynomolgus monkeys Liver microsomeIn VitroNoneNoneN.A.
4208
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis2 μM (0.5 mg protein/mL of each species pooled together)20.3Human Liver Microsome proteaseLC-MS/MSHuman Liver MicrosomeIn VitroNoneNoneN.A.
4209
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) <15CD-1 mouse Hepatocytes Lysate ProteaseLC-MS/MSCD-1 mouse Hepatocytes LysateIn VitroNoneNoneEnzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4210
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 5.81SD rats Hepatocytes Lysates proteaseLC-MS/MSSD rats hepatocytes LysatesIn VitroNoneNoneN.A.
4211
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 10.7Beagle dogs Hepatocytes Lysates proteaseLC-MS/MSBeagle dogs Hepatocytes LysatesIn VitroNoneNoneN.A.
4212
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 12.1Cynomolgus monkeys Hepatocytes Lysates proteaseLC-MS/MSCynomolgus monkeys Hepatocytes LysatesIn VitroNoneNoneN.A.
4213
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 5.28Human Hepatocytes Lysates proteaseLC-MS/MSHuman HepatocytesIn VitroNoneNoneEnzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4214
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 5.28Human Hepatocytes Lysates proteaseLC-MS/MSHuman Hepatocytes LysatesIn VitroNoneNoneEnzyme Activity = 3.18 at 2 microMolar of HM1010 (Cytochrome P450 (CYP2B6) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4215
373732032023
LRKLRKRLLRLVGRQLEEFL
HM-10/1020FreeFreeLinearLNoneChimeric high-density lipoprotein mimetic peptideAnticancerAt the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis2 μM (0.5 million cells/mL, of each species pooled together) 5.28Human Hepatocytes Lysates proteaseLC-MS/MSHuman Hepatocytes LysatesIn VitroNoneNoneEnzyme Activity = 2.06 at 2 microMolar of HM1010 (Cytochrome P450 (CYP3A4) Induction in Single-Donor Human Hepatocytes Lot HH1086)
4216
370941322023
GQWHCTTSFPHHYCLY-Bip
SNIO–CBP16Single nanometer iron oxide and PEG conjugation at N terminalAmidationCyclic (C5-C14 Disulfide Bond)LNoneSINO-CBP productUsed in detection of Liver FibrosisN.A.2 nmol/g animal5.7 ± 1.9 (Elimination Half Life)Mice blood proteaseDynamic T1-weighted MRIMice bloodIn VivoNoneNoneKd = 18.4 µM (Binding affinity of SNIO–CBP toward human type I collagen)
4217
370734942023
pGlu-LTPTPNW(Man)GT
Carmo‐HrTH‐I10pGlu = PyroglutamateAmidationLinearLC‐mannosylated tryptophan residue at position 8Derived from the corpora cardiaca (CC) of the Indian stick insect Carausius morosusHypertrehalosemia In Ligated Stick Insects0, 2‐, 5‐, 10‐and 30 min at Room temp100 pmol5C.Morosus hemolymph proteaseHPLCC.Morosus hemolymphIn VitroNoneNone[Lipid]T0 min(µg/µL) = 9.32 ± 1.59 for Natural Carmo‐HrTH‐I (10 pmol) (Biological activity of a crude methanolic extract of corpora cardiaca (CC) from the natural hypertrehalosemic hormones (HrTHs) extracted from the CC of the Indian stick insect(Carausius morosus) in an in vivo bioassay withL. migratoria)
4218
370475882023
VIKLSGRELVRAQIAISGMSTWSKRSL
B7-3327FreeFreeLinearLNoneDerived as a single-chain peptidomimetic of the B-chain of H2 relaxinTreatment of Acute Cardiac FailureA total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min)400 µg/mL6Human serum proteaseRP-HPLCHuman serumIn VitroNoneNoneHEK-7BP Binding B.S.A. Free Eu-H2 pKi = 7.28 ± 0.11
4219
370475882023
VIKLSGRELVRAQIAISGMSTWSKRSL
AcK(PalmGlu)-PEG12-B7-3327Ac modifed Lysine in Palmitic fatty acid linked with B7-33 using PEG linkerFreeLinearLNoneB7-33 analogTreatment of Acute Cardiac FailureA total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min)400 µg/mL60Human serum proteaseRP-HPLCHuman serumIn VitroNoneNoneHEK-7BP Binding B.S.A. Free Eu-H2 pKi =7.52 ± 0.13
4221
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice1.5 mg/kg0.306Mouse plasma proteaseLC-MS/MSMouse plasmaIn VivoNoneNoneN.A.
4222
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice4.5 mg/kg0.344Mouse plasma proteaseLC-MS/MSMouse plasmaIn VivoNoneNoneN.A.
4223
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice13.5 mg/kg0.547Mouse plasma proteaseLC-MS/MSMouse plasmaIn VivoNoneNoneN.A.
4224
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice1 mg/kg0.805Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4225
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice1 mg/kg0.248Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4226
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice5 mg/kg0.46Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4227
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice5 mg/kg0.437Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4228
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice75 mg/kg0.341Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4229
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice75 mg/kg0.391Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4230
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice1 mg/kg0.665Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4231
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice1 mg/kg0.668Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4232
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice5 mg/kg0.655Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4233
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice5 mg/kg0.648Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4234
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice75 mg/kg0.615Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4235
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice75 mg/kg0.62Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
4236
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice5 mg/kg0.888Monkeys Plasma ProteaseLC-MS/MSMonkeys plasma In VivoNoneNoneN.A.
4237
369827732023
CRGDKGPDC
CEND-19FreeFreeCyclic (C1-C9 Disulfide Bond)LNoneiRGD cyclic peptideAntitumorBlood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice50 mg/kg0.956Monkeys Plasma ProteaseLC-MS/MSMonkeys plasma In VivoNoneNoneN.A.
4250
366319712023
VDKPPYLPRPRPPROIYNO
Onc7219FreeAmidation, Orn=Ornithine at position 19LinearLOrn=Ornithine at position 15OncocinsAntimicrobialProdrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration4.34 mmol/kg43CD-1 mice plasma proteaseLC-MSCD-1 mice plasma In VivoNoneNone(Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113
4251
366319712023
VDKPPYLPRPRPPROIYNO
Onc7219FreeAmidation, Orn=Ornithine at position 19LinearLOrn=Ornithine at position 15OncocinsAntimicrobialProdrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration4.34 mmol/kg43CD-1 mice plasma proteaseLC-MSCD-1 mice plasma In VivoNoneNone(Onc72 in 25% mouse serum ) MIC = 25 μmol L−1 (58 mg L−1) on E.coli BW25113
4252
366319712023
VDKPPYLPRPRPPROIYNO
Onc7219FreeAmidation, Orn=Ornithine at position 19LinearLOrn=Ornithine at position 15OncocinsAntimicrobialProdrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration4.34 mmol/kg43CD-1 mice plasma proteaseLC-MSCD-1 mice plasma In VivoNoneNoneOnc72 Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS)
4253
366319712023
VDKPPYLPRPRPPROIYNO
Onc7219FreeAmidation, Orn=Ornithine at position 19LinearLOrn=Ornithine at position 15OncocinsAntimicrobialProdrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration4.34 mmol/kg43CD-1 mice plasma proteaseLC-MSCD-1 mice plasma In VivoNoneNoneOnc72: Non-toxic to human HepG2 and HEK293 cell lines at 50 μmol L−1
4272
365092202023
KLLKINLKALAALAKKIL
KM8 18FreeAmidationLinearLNoneAnalogue of MastoparanAntitumorN.A.N.A.30Mouse plasma proteasePlasma stability assayMouse plasmaIn VivoNoneNoneN.A.
4273
364107922023
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLNoneGLP-2 analogueSmall Bowel Hypertrophic EffectBlood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912670 nmol/kg0.6 ± 0.1SD rats serum proteaseGLP-2 ELISASD rats serumIn VivoNoneNoneEC50 = 0.12 ± 0.056 nM for teduglutide peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP)
4305
N.A.2023
GSSFLSPEHQRVQQRKESKKPPAKLQPR
SEQ ID NO 128FreeFreeLinearLNoneHuman Ghrelin AnalogGhrelin Receptor AgonistSolutions were incubated at 37 C for 60, 120 and 180 Minutes1 mg/ml0.2Plasma proteaseLC-MSDiluted plasma In VitroNoneEP 2023054305 WEC50(nM) = 0.83
4388
373299002023
N.A.
KAN-101N.A.N.A.N.A.N.A.N.A.Liver-targeting glycosylation signature conjugated to a deaminated gliadin peptideN.A.Liver-Targeted Immune Tolerance TherapyN.A.0·15 mg/kg, 0·3 mg/kg, 0·6 mg/kg, 1·2 mg/kg, 1·5 mg/kg3·72 to 31·72 Human proteaseN.A.HumanIn VivoNoneNoneN.A.
4395
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration20 μg/kg15.2SD rats plasma proteaseLC-MS/MSSD rats plasma In VivoNoneNoneN.A.
4396
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from rats in group five before the last three doses and within 6 h after the last dose100 μg/kg18.5SD rats plasma proteaseLC-MS/MSSD rats plasma dosed with BPC once a day for seven consecutive daysIn VivoNoneNoneN.A.
4397
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration20 μg/kg7.87SD rats plasma proteaseLC-MS/MSSD rats plasma In VivoNoneNoneN.A.
4398
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from rats in group five before the last three doses and within 6 h after the last dose100 μg/kg17.1SD rats plasma proteaseLC-MS/MSSD rats plasma dosed with BPC once a day for seven consecutive daysIn VivoNoneNoneN.A.
4399
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration500 μg/kg29.7SD rats plasma proteaseLC-MS/MSSD rats plasma In VivoNoneNoneN.A.
4400
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration6 μg/kg5.27 ± 2.25Beagle Dogs Plasma ProteaseLC-MS/MSbeagle dogs plasmaIn VivoNoneNoneN.A.
4401
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing30 μg/kg19.6 ± 3.72Beagle Dogs Plasma ProteaseLC-MS/MSbeagle dogs plasma with repeated dose of 30 μg/kg for seven consecutive daysIn VivoNoneNoneN.A.
4402
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration6 μg/kg20.0 ± 5.53Beagle Dogs Plasma ProteaseLC-MS/MSbeagle dogs plasmaIn VivoNoneNoneN.A.
4403
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration30 μg/kg25.5 ± 7.08Beagle Dogs Plasma ProteaseLC-MS/MSbeagle dogs plasmaIn VivoNoneNoneN.A.
4404
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTreatment of various wounds in rats and dogsBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration150 μg/kg29.3 ± 5.06Beagle Dogs Plasma ProteaseLC-MS/MSbeagle dogs plasmaIn VivoNoneNoneN.A.
4406
365592782022
PCKNFFWKTFSSCK
Native CST14FreeFreeCyclic (C2-C13 Disulfide Linkage)LNoneNeuropeptideAntiinflammatory37 °C6 mg/mL2Human plasma proteaseN.A.Human plasmaIn Vitrohttps://pmc.ncbi.nlm.nih.gov/articles/PMC7994712/NoneIC50(nM) = 1.7 (relative affinities of CST for the different Somatostatin receptor SSTR1)
4407
365592782022
PCKNFFWKTFSSCK
Native CST14FreeFreeCyclic (C2-C13 Disulfide Linkage)LNoneNeuropeptideAntiinflammatory37 °C6 mg/mL2Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 0.09 (relative affinities of CST for the different Somatostatin receptor SSTR2)
4408
365592782022
PCKNFFWKTFSSCK
Native CST14FreeFreeCyclic (C2-C13 Disulfide Linkage)LNoneNeuropeptideAntiinflammatory37 °C6 mg/mL2Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR3)
4409
365592782022
PCKNFFWKTFSSCK
Native CST14FreeFreeCyclic (C2-C13 Disulfide Linkage)LNoneNeuropeptideAntiinflammatory37 °C6 mg/mL2Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 0.2 (relative affinities of CST for the different Somatostatin receptor SSTR4)
4410
365592782022
PCKNFFWKTFSSCK
Native CST14FreeFreeCyclic (C2-C13 Disulfide Linkage)LNoneNeuropeptideAntiinflammatory37 °C6 mg/mL2Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR1)
4411
365592782022
PCKN-Mesityl-AFwKTFSSCK
CST analogue 514N-octanoylFreeCyclic (C2-C13 Disulfide Linkage)Mixw=D-Trp,MesitylCST analogueAntiinflammatory37 °C6 mg/mL21Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 47.3 (relative affinities of A5 for the different Somatostatin receptor SSTR1)
4412
365592782022
PCKN-Mesityl-AFwKTFSSCK
CST analogue 514N-octanoylFreeCyclic (C2-C13 Disulfide Linkage)Mixw=D-Trp,MesitylCST analogueAntiinflammatory37 °C6 mg/mL21Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 35 (relative affinities of A5 for the different Somatostatin receptor SSTR2)
4413
365592782022
PCKN-Mesityl-AFwKTFSSCK
CST analogue 514N-octanoylFreeCyclic (C2-C13 Disulfide Linkage)Mixw=D-Trp,MesitylCST analogueAntiinflammatory37 °C6 mg/mL21Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 5.1 (relative affinities of A5 for the different Somatostatin receptor SSTR3)
4414
365592782022
PCKN-Mesityl-AFwKTFSSCK
CST analogue 514N-octanoylFreeCyclic (C2-C13 Disulfide Linkage)Mixw=D-Trp,MesitylCST analogueAntiinflammatory37 °C6 mg/mL21Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 4.1 (relative affinities of A5 for the different Somatostatin receptor SSTR4)
4415
365592782022
PCKN-Mesityl-AFwKTFSSCK
CST analogue 514N-octanoylFreeCyclic (C2-C13 Disulfide Linkage)Mixw=D-Trp,MesitylCST analogueAntiinflammatory37 °C6 mg/mL21Human plasma proteaseN.A.Human plasmaIn VitroNoneNoneIC50(nM) = 1.12 (relative affinities of A5 for the different Somatostatin receptor SSTR1)
4416
365578502022
pGlu-HWSYlLRP 
Leuprolide9pGlu = PyroglutamateNHEt (Ethylamine)LinearMixd-Leucine6 substituitions SyntheticAnticancer (Treatment of Advanced Prostate Cancer)Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min)0.1 mg/kg38.2 ± 4.3 (Terminal Elimination Half Life)Male SD Rats Plasma ProteaseUPLC-MS/MSMale SD rats plasmaIn VivoNoneNoneN.A.
4419
364993572022
ILRWSRKLPCVS
JM#2112FreeFreeLinearLCysteine was introduced at position 10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM1.7Human plasma proteaseFlow cytometry-based functional assay and mass spectrometryHuman plasmaIn VitroNoneNoneN.A.
4421
364993572022
ILRWSRKLPCVS
JM#2112FreeFreeLinearLCysteine was introduced at position 10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM7Human plasma proteaseAntibody-competition assayHuman plasmaIn VitroNoneNoneN.A.
4422
364993572022
IVRWSKKVPCVS
WSC0212FreeFreeLinearLCysteine was introduced in the sequence of both peptides at position 10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM9Human plasma proteaseFunctional stability assayHuman plasmaIn VitroNoneNoneN.A.
4423
364993572022
IVRWSKKVPCVS
WSC02 12FreeFreeLinearLCysteine was introduced in the sequence of both peptides at position 10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM6Human plasma proteaseFunctional stability assayHuman plasma after GuHCl + DTT treatmentIn VitroNoneNoneN.A.
4424
364993572022
ILRWSRKLPCVS
JM#2112FreeFreeLinearLCysteine was introduced at position 10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM5Human plasma proteaseMass spectrometryHuman plasma after GuHCl + DTT treatmentIn VitroNoneNoneN.A.
4425
364993572022
IVRWSKKVPSVS
WSC02 (C10S)12FreeFreeLinearLCys10 replaced by Ser10SyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM4Human plasma proteaseMass spectrometryHuman plasmaIn VitroNoneNoneN.A.
4426
364993572022
IVRWSKKVPCVS
WSC02 (Cdm)12FreeFreeLinearLCarbamidomethylation of Cys10 residue = CdmSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM5Human plasma proteaseMass spectrometryHuman plasmaIn VitroNoneNoneN.A.
4427
364993572022
ILRWSRKLPSVS
JM#21 (C10S)12FreeFreeLinearLCys replaced by SerSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM4Human plasma proteaseMass spectrometryHuman plasmaIn VitroNoneNoneN.A.
4428
364993572022
ILRWSRKLPCVS
JM#21 (Cdm)12FreeFreeLinearLCarbamidomethylation of Cys residue = CdmSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min7 µM3Human plasma proteaseMass spectrometryHuman plasmaIn VitroNoneNoneN.A.
4429
364993572022
IVRWSKKVPCVS
WSC02 (Cdm)12FreeFreeLinearLCarbamidomethylation of Cys residue = CdmSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min20 µM6Human plasma proteaseFunctional stability assayHuman plasmaIn VitroNoneNoneN.A.
4430
364993572022
IVRWSKKVPSVS
WSC02 (C10S)12FreeFreeLinearLCys replaced by SerSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min20 µM7Human plasma proteaseFunctional stability assayHuman plasmaIn VitroNoneNoneN.A.
4431
364993572022
ILRWSRKLPCVS
JM#21 (Cdm)12FreeFreeLinearLCarbamidomethylation of Cys residue = CdmSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min20 µM3Human plasma proteaseFunctional stability assayHuman plasmaIn VitroNoneNoneN.A.
4432
364993572022
ILRWSRKLPSVS
JM#21 (C10S)12FreeFreeLinearLCys replaced by SerSyntheticAnticancer, AntiinflammatoryFive microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min20 µM4Human plasma proteaseFunctional stability assayHuman plasmaIn VitroNoneNoneN.A.
4437
364432912022
FSSE
Entry 1 (aka P5779)4FreeAmidationLinearLNoneSyntheticInhibitor of Hmgb1/Md-2/Tlr4 Complex FormationAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.0 ± 0.1C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneHMGb1:MD-2 inhibition (IC50) = 68.5 nM
4440
364432912022
FSS-azaE
Entry 4 (Azapeptide 53)4FreeAza-glutamic acid (azaE4) modification at position 4 (E4)LinearLNoneP5779 analoguesInhibitor of Hmgb1/Md-2/Tlr4 Complex FormationAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.6 ± 0.11C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneHMGb1:MD-2 inhibition (IC50) = 396.8 nM
4442
364432912022
azaF-SSQ
Entry 6 (Azapeptide 55)4Aza-Phe at postion 1Amidation, Q amino acid subtituition at place of E at C terminalLinearLNoneP5779 analoguesInhibitor of Hmgb1/Md-2/Tlr4 Complex FormationAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml24.4 ± 1.6C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneHMGb1:MD-2 inhibition (IC50) = 159.3 nM
4445
364432912022
FSS-azaQ
Entry 9 (Azapeptide 58)4FreeAmidation, Aza-glutamine (azaQ4) LinearLNoneP5779 analoguesInhibitor of Hmgb1/Md-2/Tlr4 Complex FormationAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.9 ± 0.20C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneHMGb1:MD-2 inhibition (IC50) = 422.9 nM
4446
364432912022
RPPGFSPFR
Entry 1 (Bradykinin)9FreeFreeLinearLNoneDerived from kininogen Effects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml5.29 ± 0.5C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneEC50(nM) = 44.4 (PEG2 induction in Fibroblasts)
4447
364432912022
azaR-PPGFSPFR
Entry 2 (azaR1-BK)9Modified at position 1 with an aza-amino acid (aza-arginine)FreeLinearLNoneAza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.46 ± 0.05C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4448
364432912022
R-azaP-PGFSPFR
Entry 3(azaP2-BK)9FreeFreeLinearLModified at position 2 with an aza-amino acid (aza-proline)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml5.40 ± 1.1C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneEC50(nM) = 61.1 (PEG2 induction in Fibroblasts)
4449
364432912022
RP-azaP-GFSPFR
Entry 4 (azaP3-BK)9FreeFreeLinearLModified at position 3 with an aza-amino acid (aza-proline)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.63 ± 0.25C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4450
364432912022
RPP-azaG-FSPFR
Entry 5 (azaG4-BK)9FreeFreeLinearLModified at position 4 with an aza-amino acid (aza-glycine)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml4.33 ± 1.3C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4451
364432912022
RPPG-azaF-SPFR
Entry 6 (azaF5-BK)9FreeFreeLinearLModified at position 5 with an aza-amino acid (aza-phenylalanine)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml14.7 ± 1.6C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4452
364432912022
RPPGFS-azaP-FR
Entry 7 (azaP7-BK)9FreeFreeLinearLModified at position 7 with an aza-amino acid (aza-proline)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml2.38 ± 0.03C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4453
364432912022
RPPGFSP-azaF-R
Entry 8 (azaF8-BK)9FreeFreeLinearLModified at position 8 with an aza-amino acid (aza-phenylalanine)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml39.3 ± 2.5C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneEC50(nM) = 99.6 (PEG2 induction in Fibroblasts)
4454
364432912022
RPPGFSPF-azaR
Entry 9 (azaR9-BK)9FreeFreeLinearLModified at position 9 with an aza-amino acid (aza-arginine)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml42.6 ± 0.8C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneN.A.
4455
364432912022
R-azaP-PGFSP-azaF-R
Entry 10 ([azaP2, azaF8]-BK)9FreeFreeLinearLModified at both positions 2 and 8 with aza-amino acids (aza-proline and aza-phenylalanine, respectively)Aza-bradykinin analoguesEffects on Pain, Inflammation, Edema/Vasodilation and Blood PressureAliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes)0.1 mg/ml29.2 ± 3.8C57Bl/6 J mouse serum proteaseLC-MS/MSC57BL/6 J male mouse serumIn VitroNoneNoneEC50(nM) = 80.6 (PEG2 induction in Fibroblasts)
4457
363809172022
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneGlucagonAntidiabetes37 °C0.3 nmol10.2 ± 0.4 DPP-IVRP-HPLC50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV In VitroPDB id: 5VAINoneBGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) 
4458
363809172022
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneGlucagonAntidiabetes37 °C6 nmol55.7 ± 12.1Mouse serum proteaseRP-HPLCMouse serumIn VitroPDB id: 5VAINoneBGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability)
4459
363809172022
HAEGTFTSNVSSYLEGQAAKEFIAWLVKGRG
Glc-GLP-1-131FreeFreeLinearLGlucosylation at Asn15GLP-1 analogsAntidiabetes37 °C0.3 nmol 30.2 ± 2.4 DPP-IVRP-HPLC50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV In VitroNoneNoneN.A.
4461
363809172022
HAEGTFTSDVSSYLEGQAANESIAWLVKGRG
Glc-GLP-1-331FreeFreeLinearLGlucosylation at Asn26GLP-1 analogsAntidiabetes37 °C0.3 nmol 46.1 ± 3.5 DPP-IVRP-HPLC50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV In VitroNoneNoneN.A.
4463
363809172022
HAEGTFTSDVSSYLEGQAAKEFIAWLVNGTG
Glc-GLP-1-531FreeFreeLinearLGlucosylation at Asn34GLP-1 analogsAntidiabetes37 °C0.3 nmol 32.5 ± 1.4 DPP-IVRP-HPLC50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV In VitroNoneNoneN.A.
4465
363809172022
HAEGTFTSNVSSYLEGQAAKEFIAWLVKGRG
Glycan-GLP-1-1(G2)31FreeFreeLinearLN-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan)GLP-1 analogsAntidiabetes37 °C0.3 nmol 49.1 ± 5.7 DPP-IVRP-HPLC50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV In VitroNoneNoneBGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) 
4497
361350982022
QDTDTWA
GNRs-AAP1-Cy57FreeFreeLinearLCy5 conjugationAAP1/AAP1-1/AAP1-2 modified GNRsAntiadhesive propertyAt 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution 1 mg/ml0.29 (T1/2 a)Mouse serum proteaseHPLC1 mL mouse serum In VitroNoneNoneN.A.
4499
361350982022
WTDAQTD
GNRs-AAP1-1-Cy57FreeFreeLinearLCy5 conjugationAAP1/AAP1-1/AAP1-2 modified GNRsAntiadhesive propertyAt 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution 1 mg/ml0.18 (T1/2 a)Mouse serum proteaseHPLC1 mL mouse serum In VitroNoneNoneN.A.
4501
361350982022
TADWTDQ
GNRs-AAP1-2-Cy57FreeFreeLinearLCy5 conjugationAAP1/AAP1-1/AAP1-2 modified GNRsAntiadhesive propertyAt 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution 1 mg/ml0.2 (T1/2 a)Mouse serum proteaseHPLC1 mL mouse serum In VitroNoneNoneN.A.
4503
361127712022
CP-1Nal-dCM-HArg-DWSTP-HyP-WC
BT800916AcetylationConjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10Bicyclic Mixcyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modificationBT8009 and MMAE cytotoxin hybridAnticancerN.A.1 mg/kg1Mouse plasma proteaseLC-MS/MSMouse plasmaIn VivoNoneNoneKD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse)
4504
361127712022
CP-1Nal-dCM-HArg-DWSTP-HyP-WC
BT800916AcetylationConjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10Bicyclic Mixcyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modificationBT8009 and MMAE cytotoxin hybridAnticancerN.A.1 mg/kg0.9Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneKD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat)
4518
361014522022
YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
AM52FreeAmidationCyclic (C16-C21 Disulfide Bond)LNoneIsolated from Human pheochromocytomaVasodilator and Cardiovascular ProtectionBlood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration50 nmol/kg32.3Wistar rats plasma proteaseELISA (measure mAM )Wistar rats plasmaIn VivoNoneNoneAfter treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4519
361014522022
YRQSMNNFQGLRSFGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
AM52FreeAmidationCyclic (C16-C21 Disulfide Bond)LNoneIsolated from Human pheochromocytomaVasodilator and Cardiovascular ProtectionBlood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration50 nmol/kg27.5Wistar rats plasma proteaseELISA (measure tAM )Wistar rats plasmaIn VivoNoneNoneAfter treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group
4525
360348082022
MGHPPLLPLLLLLHTCVPASWGLRCMQCKTNGDCRVEECALGQDLCRTTIVRLWEEGEELELVEKSCTHSEKTNRTLSYRTGLKITSLTEVVCGLDLCNQGNSGRAVTYSRSRYLECISCGSSDMSCERGRHQSLQCRSPEEQCLDVVTHWIQEGEEGRPKDDRHLRGCGYLPGCPGSNGFHNNDTFHFLKCCNTTKCNEGPILELENLPQNGRQCYSCKGNSTHGCSSEETFLIDCRGPMNQCLVATGTHEPKNQSYMVRGCATASMCQHAHLGDAFSMNHIDVSCCTKSGCNHPDLDVQYRSGAAPQPGPAHLSLTITLLMTARLWGGTLLWT
uPAR335FreeFreeLinearLNoneDerived from PLAUR genePlays role in thrombosisN.A.N.A.48.2 ± 2.3 BEAS-2B cells lysate proteaseDensitometry analysis using NIH Image JBEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + CycloheximideIn VivoNoneNoneN.A.
4546
358902242022
K-(PEG)4-E
177Lu-Palm-3PRGD22Lys1 linked with (palmitoyl-Glu-OH)Glu3 linked with (PEG4-c(RGDfK))2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in betweenSyntheticAntitumorN.A.0.74 MBq4.49 (T1/2a)KM mice blood proteaseGamma counterKM mice blood sampleIn VivoNoneNoneN.A.
4547
358902242022
E
177Lu-3PRGD21PEG4Glu linked with [PEG4-c(RGDfK)]2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4SyntheticAntitumorN.A.0.74 MBq1.94 (T1/2a)KM mice blood proteaseGamma counterKM mice blood sampleIn VivoNoneNoneN.A.
4549
358902242022
E
177Lu-3PRGD21PEG4Glu linked with [PEG4-c(RGDfK)]2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4SyntheticAntitumorN.A.0.74 MBq11.81 (T1/2Β) KM mice blood proteaseGamma counterKM mice blood sampleIn VivoNoneNoneN.A.
4551
358902242022
E
177Lu-3PRGD21PEG4Glu linked with [PEG4-c(RGDfK)]2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4SyntheticAntitumorN.A.0.74 MBq14.54 (Slow)C57Bl/6 mice blood proteaseGamma counterC57BL/6 mice blood sampleIn VivoNoneNoneN.A.
4552
358902242022
K-(PEG)4-E
177Lu-Palm-3PRGD22Lys1 linked with (palmitoyl-Glu-OH)Glu3 linked with (PEG4-c(RGDfK))2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in betweensyntheticAntitumorN.A.0.74 MBq2.08 (Fast)C57Bl/6 mice blood proteaseGamma counterC57BL/6 mice blood sampleIn VivoNoneNoneN.A.
4553
358902242022
E
177Lu-3PRGD21PEG4Glu linked with [PEG4-c(RGDfK)]2Cyclic (3PRGD2)Mix177Lu radiolabeling at PEG4syntheticAntitumorN.A.0.74 MBq1.06 (Fast)C57Bl/6 mice blood proteaseGamma counterC57BL/6 mice blood sampleIn VivoNoneNoneN.A.
4568
358075002022
AEWCP
TIPP5FreeFreeLinearLNoneFrom calf thymus extractsTreatment of AsthmaAt 0.5, 1, 2, 5, 10, 15, 20, and 40 min post administration (eight mice at each time points), blood samples were taken from an inner canthus 50 mg/kg5.99 ± 1.82Mice plasma proteaseLC-MS/MSMice plasmaIn VivoNoneNoneTIPP inhibits degranulation and inflammation in RBL-2H3 cells and pretreatment with 200 microgram/mL of TIPP for 20 minutes reduces the level of biomarkers of allergic response and inflammation i.e β-hexosaminidase, Histamine, IL-4
4569
357791892022
WSGWSSCSRSCG
NX21012FreeFreeLinearLNoneDerived from the subcommissural organ (SCO)-spondinTreatment of Neurodegenerative Diseases Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion2.5 mg/kg13.3Human plasma proteaseHPLC–MS/MSHuman plasma In Vivohttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC3965545/NoneN.A.
4570
357791892022
WSGWSSCSRSCG
NX21012FreeFreeLinearLNoneDerived from the subcommissural organ (SCO)-spondinTreatment of Neurodegenerative Diseases Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion5 mg/kg6.19Human plasma proteaseHPLC–MS/MSHuman plasma In VivoNoneNoneN.A.
4571
357791892022
WSGWSSCSRSCG
NX21012FreeFreeLinearLNoneDerived from the subcommissural organ (SCO)-spondinTreatment of Neurodegenerative Diseases Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion10 mg/kg20Human plasma proteaseHPLC–MS/MSHuman plasma In VivoNoneNoneN.A.
4575
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.04 mmol/kg0.3 (Elimination Half Life)Male SD rats plasma proteaseICP-MSMale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4576
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.04 mmol/kg0.28 (Elimination Half Life)Female SD rats plasma proteaseICP-MSFemale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4577
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.04 mmol/kg0.57(Elimination Half Life)(P) SD rats plasma proteaseICP-MS(P) SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4578
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.1 mmol/kg0.31 (Elimination Half Life)Male SD rats plasma proteaseICP-MSMale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4579
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.1 mmol/kg0.32 (Elimination Half Life)Female SD rats plasma proteaseICP-MSFemale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4580
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.1 mmol/kg0.65 (Elimination Half Life)(P) SD rats plasma proteaseICP-MS(P) SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4581
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.2 mmol/kg0.3 (Elimination Half Life)Male SD rats plasma proteaseICP-MSMale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4582
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.2 mmol/kg0.32 (Elimination Half Life)Female SD rats plasma proteaseICP-MSFemale SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4583
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 30.2 mmol/kg0.22 (Elimination Half Life)(P) SD rats plasma proteaseICP-MS(P) SD rats plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4584
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.04 mmol/kg0.76 (Elimination Half Life)Male dogs plasma proteaseICP-MSMale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4585
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.04 mmol/kg0.74 (Elimination Half Life)Female dogs plasma proteaseICP-MSFemale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4586
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.04 mmol/kg0.8 (Elimination Half Life)(P) dogs plasma proteaseICP-MS(P) dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4587
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.1 mmol/kg0.7 (Elimination Half Life)Male dogs plasma proteaseICP-MSMale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4588
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.1 mmol/kg0.67 (Elimination Half Life)Female dogs plasma proteaseICP-MSFemale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4589
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.1 mmol/kg0.33 (Elimination Half Life)(P) dogs plasma proteaseICP-MS(P) dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4590
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.2 mmol/kg0.69 (Elimination Half Life)Male dogs plasma proteaseICP-MSMale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4591
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.2 mmol/kg0.63 (Elimination Half Life)Female dogs plasma proteaseICP-MSFemale dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4592
357034632022
TVRTSAD
MT2187FreeZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linkerLinearLNoneZD2 analogCancer targeting contrast agentBlood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3.0.2 mmol/kg0.048 (Elimination Half Life)(P) dogs plasma proteaseICP-MS(P) dogs plasmaIn VivoNoneNoneMT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM
4608
356465432022
HsQGTFTSDYSKYLDKRRAQDFVQWLLNTGGPSSGAPPPS
TB00140FreeAmidation, GGPSSGAPPPS introduced in the C-terminalCyclic (R17-D21 Lactam Bridge)MixD serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3)GLP-1 and GCG chimera analogTreatment of Multiple Causes of Hepatic FibrosisN.A.15.3 μg/kg0.498 ± 0.0100Rhesus monkeys plasma proteaseHPLC–MS/MSRhesus monkeys plasmaIn VivoNoneNoneGCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 
4631
354148772022
MVATKTFALLLLSLFLAVGLGEKKEGHFSALPSLPVGSHAKVSSPQPRGPRYAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQREARALELASQANRKEEEAVEPQSSPAKNPSDEDLLRDLLIQELLACLLDQTNLCRLRSR
Native GIP153FreeFreeLinearLNoneGlucagonGlucose dependent insulinotropic At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins1 μM45Human plasma protease LC-MS80% pooled human Li-heparin plasma In VitroNoneNoneN.A.
4632
354148772022
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneGlucagonAntidiabetesAt selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins1 μM35Human plasma protease LC-MS80% pooled human Li-heparin plasma In VitroPDB id: 5VAINoneN.A.
4638
353594942022
EMRLSKFFRDFILQRKK
CSP117FreeFreeLinearLNoneCompetence stimulating peptideModulates Quorum Sensing In Streptococcus PneumoniaeAliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points1 mM30Trypsin RP-HPLCPBS solutionIn VitroNoneNoneEC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor
4639
353594942022
EMRLSKFFRDFILQRKK
CSP117FreeFreeLinearLNoneCompetence stimulating peptideModulates Quorum Sensing In Streptococcus PneumoniaeAliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points1 mM1ChymotrypsinRP-HPLCPBS solutionIn VitroNoneNoneEC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor
4644
351806462022
YPSKPDNPGEDAPAEDMARYYSALRHYINLITRQRY
NPY1–3636FreeAmidationLinearLNoneHuman derivedVasoconstrictor168 min for a study dayN.A.4.66 ± 0.70Human plasma proteaseLC-MS/MSHuman plasma after Heavy exerciseIn VivoPDB id: 7RTANoneN.A.
4645
351806462022
YPSKPDNPGEDAPAEDMARYYSALRHYINLITRQRY
NPY1–3636FreeAmidationLinearLNoneHuman derivedVasoconstrictor168 min for a study dayN.A.4.78 ± 1.07Human plasma proteaseLC-MS/MSHuman plasma with 5 mg saxagliptin after Heavy exerciseIn VivoPDB id: 7RTANoneN.A.
4646
351806462022
SKPDNPGEDAPAEDMARYYSALRHYINLITRQRY
NPY3–3634FreeAmidationLinearLNoneHuman derivedVasoconstrictor168 min for a study dayN.A.26.9 ± 6.2Human plasma proteaseLC-MS/MSHuman plasma after Heavy exerciseIn VivoPDB id: 7RTANoneN.A.
4647
351806462022
SKPDNPGEDAPAEDMARYYSALRHYINLITRQRY
NPY3–3634FreeAmidationLinearLNoneHuman derivedVasoconstrictor168 min for a study dayN.A.25.5 ± 6.2 Human plasma proteaseLC-MS/MSHuman plasma with 5 mg saxagliptin after Heavy exerciseIn VivoPDB id: 7RTANoneN.A.
4649
351746982022
MVSKGEELFTGVVPILVELDGDVNGHKFSVSGEGEGDATYGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKQHDFFKSAMPEGYVQERTIFFKDDGNYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNYNSHNVYIMADKQKNGIKVNFKIRHNIEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSALSKDPNEKRDHMVLLEFVTAAGITLGMDELYK-AANDENYALAA
GFP-Ec250GFPEc (E.coli) SsrA tag sequences conjugationLinearLNoneeGFP derivativeIncreases Half LifeN.A.N.A.6E. Coli Bl21(De3) cells lysate proteaseFluorescence assayE. coli BL21(DE3) cells lysate after 5 h removed the inducerIn VivoPDB id: 4EULNoneN.A.
4650
351746982022
MVSKGEELFTGVVPILVELDGDVNGHKFSVSGEGEGDATYGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKQHDFFKSAMPEGYVQERTIFFKDDGNYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNYNSHNVYIMADKQKNGIKVNFKIRHNIEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSALSKDPNEKRDHMVLLEFVTAAGITLGMDELYK-AANKNEENTNEVPTFMLNAGQANYAFA
GFP-Mf266GFPMf (M.fluorum) SsrA tag sequencesLinearLNoneeGFP derivativeIncreases Half LifeN.A.N.A.56E. Coli Bl21(De3) cells lysate proteaseFluorescence assayE. coli BL21(DE3) cells lysate after 5 h removed the inducerIn VivoPDB id: 4EULNoneN.A.
4652
351746982022
MVSKGEELFTGVVPILVELDGDVNGHKFSVSGEGEGDATYGKLTLKFICTTGKLPVPWPTLVTTLTYGVQCFSRYPDHMKQHDFFKSAMPEGYVQERTIFFKDDGNYKTRAEVKFEGDTLVNRIELKGIDFKEDGNILGHKLEYNYNSHNVYIMADKQKNGIKVNFKIRHNIEDGSVQLADHYQQNTPIGDGPVLLPDNHYLSTQSALSKDPNEKRDHMVLLEFVTAAGITLGMDELYK-AANDENYALAA
GFP-Ec250GFPEc (E.coli) SsrA tag sequencesLinearLNoneeGFP derivativeIncreases Half LifeN.A.N.A.14E. Coli Bl21(De3) star strain lysate proteaseFluorescence assayE. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out In VivoPDB id: 4EULNoneN.A.
4654
351508052022
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection1200 nmol/kg0.137 (Terminal Half Life)Male CDR1 mice plasma proteaseELISAMale CDR1 mice plasmaIn VivoPDB id: 7MLLNoneEC50 = 0.42nM ( in the classical in vitro GLP1R cell based assay based on cAMP)
4662
351135752022
ETVTLLVALKVRYRERIT-Ahx-CKRGARSTC
TT1-IP peptide27FreeAmidationCyclic (C-C Disulfide Bond)LConjugation of TT1 and IP proteins which is linked by AhxTT1 and IP fusion proteinAntitumor (Effect on TPP-IPs on Cll xenograft models)plasma collected at 10, 20, 30, 45, 60, 120 and 360 min5 mg/kg28 (Terminal Half Life)BALB/c mice plasma proteaseHPLC-MSBalb/c mice plasmaIn VivoNoneNoneThe average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days)
4671
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment of Ischemic StrokeBlood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion1 mg0.25 ± 0.02Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4672
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment of Ischemic StrokeBlood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion4 mg0.36 ± 0.04Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4673
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment of Ischemic StrokeBlood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion10 mg0.45 ± 0.05Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4674
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment of Ischemic StrokeBlood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion20 mg0.55 ± 0.07 Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4675
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment Of Ischemic Strokeblood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion30 mg0.70 ± 0.08Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4676
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment Of Ischemic Strokeblood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion45 mg0.73 ± 0.05Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4677
349540522022
KEIVSRNKRRYQEDGRKKRRQRRR
SY-00724FreeFreeLinearLNoneNeuropeptideTreatment Of Ischemic Strokeblood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion60 mg0.78 ± 0.06Human plasma protease LC-MSHuman plasmaIn VivoNoneNoneN.A.
4678
349104922022
SETSKSF
68Ga-DOTA-SETSKSF768Ga labelledFreeCyclicLNoneSyntheticUsed For Positron Emission Tomography imaging of PD-L1 expression in tumorsN.A.N.A.14.48 ± 3.26N.A.N.A.N.A.N.A.NoneNoneN.A.
4689
344310712022
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
vosoritide39FreeFreeCyclic (Cysteine (23->39)-Disulfide)LNoneAnalog of C-type natriuretic peptideTreatment of AchondroplasiaIn a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose15 µg/kg 24.4Human plasma protease ELISAHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-StructureNoneN.A.
4690
344310712022
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
vosoritide39FreeFreeCyclic (Cysteine (23->39)-Disulfide)LNoneAnalog of C-type natriuretic peptideTreatment of AchondroplasiaIn a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose30 µg/kg 27Human plasma protease ELISAHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-StructureNoneN.A.
4691
344310712022
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
vosoritide39FreeFreeCyclic (Cysteine (23->39)-Disulfide)LNoneAnalog of C-type natriuretic peptideTreatment of AchondroplasiaIn the phase III study, full PK sampling was performed at day 1 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose15 µg/kg21Human plasma protease ELISAHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-StructureNoneN.A.
4692
344310712022
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
vosoritide39FreeFreeCyclic (Cysteine (23->39)-Disulfide)LNoneAnalog of C-type natriuretic peptideTreatment of AchondroplasiaIn the phase III study, full PK sampling was performed at week 26 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose15 µg/kg26.6Human plasma protease ELISAHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-StructureNoneN.A.
4693
344310712022
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
vosoritide39FreeFreeCyclic (Cysteine (23->39)-Disulfide)LNoneAnalog of C-type natriuretic peptideTreatment of AchondroplasiaIn the phase III study, full PK sampling was performed at week 52, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose15 µg/kg27.9Human plasma protease ELISAHuman plasmaIn Vivohttps://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-StructureNoneN.A.
4694
342177752022
VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
FE 99232630FreeAmidationLinearLNoneDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min0.3 mg/kg6.5 ± 1.8Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4695
342177752022
vYC-Agp-DVGPFC-3Pal
FE 99232510D-val at position 1Amidation, 3-Pal modification at C terminalCyclic (C3-C10 disulfide bond)MixAgpDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min0.3 mg/kg21 ± 2Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325
4696
342177752022
vFCODVGPFC-3Pal
FE 20503010Oxazole-2-carbonyl, D-val at position 1Amidation, 3-Pal modification at C terminalCyclic (C3-C10 disulfide bond)MixPhe linked with (2-Cbm),3Pal, Orn linked with iPrDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min0.2 mg/kg25 ± 8Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4697
342177752022
VTHRLAGLLSRSGGVVKNNFVPTNVGSKAF
FE 99232630FreeAmidationLinearLNoneDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min1 mg/kg11 ± 8.4Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4698
342177752022
vYC-Agp-DVGPFC-3Pal
FE 99232510D-val at position 1Amidation, 3-Pal modification at C terminalCyclic (C3-C10 disulfide bond)MixAgpDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min1 mg/kg48 ± 11Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325
4699
342177752022
vFCODVGPFC-3Pal
FE 20503010Oxazole-2-carbonyl, D-val at position 1AmidationCyclic (C3-C10 disulfide bond)MixPhe linked with (2-Cbm),3Pal, Orn linked with iPrDerived from CGRPTreatment of Acute Episodic MigraineBlood sample was collected at 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min0.6 mg/kg23 ± 2Male SD rats plasma proteaseLC-MS/MSMale SD rats plasmaIn VivoNoneNoneRat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030
4704
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose100 μg/kg18.5Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4705
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose20 μg/kg7.87Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4706
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose100 μg/kg17.1Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4707
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose500 μg/kg29.7Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
4708
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing6 μg/kg5.27 ± 2.25Beagle dogs plasma proteaseLC-MS/MSBeagle dogs plasmaIn VivoNoneNoneN.A.
4709
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing30 μg/kg19.6 ± 3.72Beagle dogs plasma proteaseLC-MS/MSBeagle dogs plasmaIn VivoNoneNoneN.A.
4710
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing6 μg/kg20.0 ± 5.53Beagle dogs plasma proteaseLC-MS/MSBeagle dogs plasmaIn VivoNoneNoneN.A.
4711
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing30 μg/kg25.5 ± 7.08Beagle dogs plasma proteaseLC-MS/MSBeagle dogs plasmaIn VivoNoneNoneN.A.
4712
365887172022
GEPPPPGKPADDAGLV
BPC15715FreeFreeLinearLNoneIsolated from human gastric juiceTherapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And FracturesBlood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing150 μg/kg29.3 ± 5.06Beagle dogs plasma proteaseLC-MS/MSBeagle dogs plasmaIn VivoNoneNoneN.A.
4713
N.A.2022
eeeeeeeeeXPLGLAGrrrrrrrrrk
12kD-PEG-e9-XPLGLAG-r9-k(cy5)2512 KDa PEGCy5 linked with Lys side chain at C terminusLinearMixe=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linkerSyntheticTransport moleculeBlood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points6 nmol20Mice blood plasma proteaseN.A.Mice blood plasmaIn VivoNoneUS 201916457763 AN.A.
4731
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFETPR-OH)
Example 1251FreeB29R, desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modification, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesBlood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes1 nmol/kg46Lyd pig plasma proteaseELISALyd pig plasmaIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 13
4741
N.A.2022
(GIVEQCCTSICSLEQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYEER-OH)
Example 451FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA14E, A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B27E, B28E modifications, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg24SD rats plasma proteaseLC-MSSD rats plasmaIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 28.6
4742
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYTDR-OH)
Example 1051FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modification, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg28SD rats plasma proteaseLC-MSSD rats plasmaIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3
4743
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFETER-OH)
Example 1151FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E, B28E modificatino, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg28SD rats plasma proteaseLC-MSSD rats plasmaIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 13.6
4744
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFETPR-OH)
Example 1251FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg25SD rats plasma proteaseLC-MSSD rats plasmaIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 13
4745
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTPR-OH)
PA251FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-gGlu-2×OEG) modificationsInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg24SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AN.A.
4746
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTDR-OH)
PA351FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)tetradecanedioyl-4×gGlu), B28D modificationsInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg26SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AN.A.
4747
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYTDR-OH)
Example 3351FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg58SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AhIGF1R 0.1% HSA (% rel to HI) Ex48 = 85.1
4749
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFETPR-OH)
Example 4151FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)hexadecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg57SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AN.A.
4750
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVEQHLCGDHLVEALYLVCGERGFFETPR-OH)
Example 4251FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B26E modifications, A and B chain linked with disulfide bondInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg41SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AN.A.
4751
N.A.2022
(GIVEQCCTSICSLYQLENYCNK*-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTPR-OH)
PA151FreeB29R, desB30 modificationCyclic (C7-C12 disulfide bond in A chain)LA22K(N(eps)hexadecanedioyl-gGlu-2×OEG) modificationInsulin Derivative AntidiabetesPlasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing25 nmol/kg41SD rats plasma proteaseLC-MSSD rats plasma with 3 Zn/Hexamer Of Insulin DerivativeIn VivoNoneUS 201615754395 AN.A.
4771
351779452022
RPRLSHKGPMPF
pE13F13pGlu = PyroglutamateFreeLinearLNoneApelin AnalogDiuretic and Cardiovascular effectsIncubated at 37°C for various times, from T0 to T4 h5 μM7.2Mouse plasma proteaseLC-MSMouse plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneKi(nM) = 0.56 ± 0.07
4773
351779452022
KFRRQRPRLSHKGPMPF
K17F17FreeFreeLinearLNoneApelin AnalogDiuretic and Cardiovascular effectsIncubated at 37°C for various times, from T0 to T4 h5 μM4.6Mouse plasma proteaseLC-MSMouse plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneKi(nM) = 0.06 ± 0.01
4774
351779452022
KFrRqRPRlS-Aib-kaP-Nle-P
P9216Lys1 acetylationFreeLinearMixD-Arg = r, D-Gln = q, D-Leu = l, D-ala = a, Proline side chain linked with (4Br-Phe) at C terminusApelin AnalogDiuretic and Cardiovascular effectsIncubated at 37°C for various times, from T0 to T4 h5 μM24Mouse plasma proteaseLC-MSMouse plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneKi(nM) = 0.09 ± 0.02
4820
352591492022
RKDVY
TP55FreeFreeLinearLNoneSyntheticTreatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids)One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration.1 mg/kg0.022 ± 0.004Wistar rats plasma proteaseLC-MS/MSWistar rats plasmaIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneThe cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5 
4843
358075582022
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneGlucagonTreatment Of Type 2 DiabetesThe reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)1 μM46Minipigs plasma proteaseLC-MSMinipigs plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/, PDB id: 5VAINoneN.A.
4844
350595682021
Hoo-FOP-hle-Pff-F
JPE-13757Hoo = L-hydroorotic acidAmidationLinearMixhle5 = D-homoleucine, Pff6 = Phe(4-F), Orn = Ornithine,Replaces the C-terminal Arg of PMX53 with a hydrophobic amino acidPeptidomimetic C5a receptor antagonistsC5Ar1 AntagonistsSerial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein 1 mg/kg0.13 (Elimination Half Life)Mice plasma proteaseLC-MSMice plasmaIn VivoNoneNoneThe inhibition of TNF levels also presented a similar median effective concentration (EC50) for PMX53 (5.9 μM) 
4846
350569792021
FRRG
Al-ProD4MaleimideDOXLinearLNoneAlbumin-binding maleimide and cathepsin B-cleavable peptide conjugateAntitumorblood samples were collected from mice at pre-determined times (0, 3 h, 6 h, 9 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h, and 144 h)3 mg/kg3.1BALB/C nude mice plasma proteaseFluorescence assayBALB/c nude mice plasmaIn VivoNoneNoneThe IC50 value of HSA-bound Al-ProD in MDA-MB231 breast cancer cells is 7.33 µM, On day 20, the tumor volume in the Al-ProD-treated group was 347.42 ± 25.9 mm³, significantly smaller than the free DOX group (580.25 ± 139.92 mm³) and saline group (1810.98 ± 544.56 mm³)
4880
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 4434FreeAmidationLinearLFatty acid conjugation at position 30Derived from PYYAntiobesityN.A.15 nmol/kg0.5Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneN.A.
4889
346613902021
VVGSPSAQDEASPLS
VVGS peptide15FreeFreeLinearLNoneSyntheticTargets tropoelastinAliquots (6 μL) taken after 0, 35, and 120 min 0.6 mM which is diluted in water at a final concentration of 0.06 mM when aliquoting45Pooled serum protease from human male AB plasmaRP-HPLC50% pooled serum from human male AB plasmaIn VitroNoneNoneKD (μM) = 41 ± 12 ( Interaction between Immobilized Human Recombinant Tropoelastin and Gd4TESMA)
4892
346303782021
GPVEDAITAAIGRVADTVGTGPTNSEAIPALTAAETGHTSQVVPGDTMQTRHVKNYHSRSESTIENFLCRSACVYFTEYENSGAKRYAEWVLTPRQAAQLRRKLEFFTYVRFDLELTFVITSTQQPSTTQNQDAQILTHQIMYVPPGGPVPDKVDSYVWQTSTNPSVFWTEGNAPPRMSIPFLSIGNAYSNFYDGWSEFSRNGVYGINTLNNMGTLYARHVNAGSTGPIKSTIRIYFKPKHVKAWIPRPPRLCQYEKAKNVNFQPSGVTTTRQSITTMTNTGAF
VP1 vaccine284FreeFreeLinearLNoneSyntheticTreatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis 1h at RT0.25 μg/μL<15Murine serum proteaseELISAMurine serumIn VivoNoneNoneABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73%
4893
345755812021
OP-(d-Cha)-WR
C5a receptor 1 antagonist (PMX205)5HC = Hydrocinnamate, O1: ornithineFreeCyclicMixD-Cha3: cyclohexylalanineLipophilic analogue of PMX53Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord InjuryBlood samples were collected at 0.04, 0.25, 0.5, 0.75, 1, 1.5, 1, 4, 6, and 24 h for both groups and then 48, 72, 96, and 120 h1 mg/kg0.84 (Terminal Elmination Half Life)Mice plasma proteaseLC-MS/MS Mice plasmaIn VivoNoneNoneIC50 = 31 nM for PMX205
4894
345755812021
OP-(d-Cha)-WR
C5a receptor 1 antagonist (PMX205)5HC = Hydrocinnamate, O1: ornithineFreeCyclicMixD-Cha3: cyclohexylalanineLipophilic analogue of PMX53Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord InjurySamples (n = 4) were quenched at regular intervals of 5 min, 10 min, 15 min, 30 min and 60 min 1 µg/ml0.17 (Elimination Half Life)Mice plasma proteaseLC-MS/MS Mice plasmaIn VivoNoneNoneIC50 = 31 nM for PMX205
4895
345755812021
OP-(d-Cha)-WR
C5a receptor 1 antagonist (PMX205)5HC = Hydrocinnamate, O1: ornithineFreeCyclicMixD-Cha3: cyclohexylalanineLipophilic analogue of PMX53Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord InjuryBlood sample was collected at 2.5, 5, 10, 15, 30, 45, 60, and 90 min1 μg/mL0.33 (Elimination Half Life)Mice spinal cord homogenate proteaseLC-MS/MS Mice spinal cord homogenateIn VivoNoneNoneIC50 = 31 nM for PMX205
4899
344550102021
pGlu-RPVNLTMRRKLRKHNCLQRRCMPLHSRVPFP
ELA-3232pGlu = PyroglutamateFreeCyclic (Cys-Cys Disulfide Bond)LNoneDerived from ZebrafishAnticancer, Treatment of Cardiovascular DiseaseBlood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120, 240 min5 μg/mL47.2 ± 5.7Human plasma proteaseLC–MS/MS Human plasmaIn VitroNoneNoneN.A.
4905
344021972021
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLNoneGLP-2 analogueTreatment of Short Bowel Syndrome N.A.0.05 mg/kg0.89Human plasma protease N.A.Human pediatrics plasma (in Japanese patients with SBS)In VivoDB id: DB08900NoneN.A.
4906
344021972021
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLNoneGLP-2 analogueTreatment of Short Bowel Syndrome N.A.0.05 mg/kg1Human plasma protease N.A.Human pediatrics plasma (in non - Japanese patients with SBS)In VivoDB id: DB08900NoneN.A.
4909
343937942021
KFRRQRPRLSHLGPMPF
LIT01-19617Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) to the N-terminal part of K17FFreeLinearLNoneApelin-17 AnalogTreatment of HypertensionN.A.900 nmol/kg28Rats plasma proteaseRIARats plasma In VivoPubchem CID Apelin: 56841713NoneIC50 = 0.56 ± 0.04 nmol/l for LIT01-196
4912
342066312021
YGGFL
Leu-ENK5FreeFreeLinearLNoneOpioid peptideAnalgesicAliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min315 µmol/L25Mice plasma proteaseUPLCMice dipotassium ethylenediaminetetraacetic acid containing pooled plasmaIn VitroNoneNoneN.A.
4916
342013982021
KRRVRWIIW
optP79FreeFreeLinearLNoneSyntheticAntimicrobialFor 0, 0.5, 1, 3, 6, and 24 h at 37 °C100 μM13Human serum proteaseUPLC-MS Human serumIn VitroNoneNoneMIC(µM) = 3 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 0.8 for E.coli in growth media MH,MIC(µM) = 1.5 for K. pneumoniae in growth media MH,MIC(µM) = 1.5 for A. baumannii in growth media MH,MIC(µM) = 0.8 for VRE in growth media MH,MIC(µM) = 6 for MRSA in growth media MH
4917
342013982021
CAAKRRVRWIIWAAC
c-optP715FreeFreeCyclic(Cys1-Cys15)LAll Alanine replaced by β-alanine SyntheticAntimicrobialFor 0, 0.5, 1, 3, 6, and 24 h at 37 °C100 μM9Human serum proteaseUPLC-MS Human serumIn VitroNoneNoneMIC(µM) = 142 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 71 for E.coli in growth media MH,MIC(µM) > 142 for K. pneumoniae in growth media MH,MIC(µM) = ND for A. baumannii in growth media MH,MIC(µM) > 142 for VRE in growth media MH,MIC(µM) = 142 for MRSA in growth media MH
4919
341633522021
YHPYKEIEQLIELANYQVLS
OPT20FreeFreeLinearLNoneDerived from the QKHPD-containing region of NCX1Binds To Pser68-PlmAliquots of 50 μl were collected at different time points (0–48 h)300 μM0.86Human serum proteaseMass spectrometryHuman serum In VitroNoneNoneN.A.
4922
341224002021
RKDVY
TP55FreeFreeLinearLNonederived from thymopoietinImmunomodulatory15 min at 37°C10 µg/mL3.2 ± 0.5Human serum proteaseHPLCHuman serum In VitroNoneNoneThe cytotoxicity of CbTP was lower than that of parental peptide CATH2
4927
361330172021
KGSGSGCPRILMRCKQDSDCLAGCVCGPNGFCG
CKP-NLP30FreeFreeLinearLAF488 labeled , Lys1 fatty acid conjugation (Palm)SyntheticPlatform for potential delivery of peptide like drug candidates37 °CN.A.1N.A.SECN.A.In VitroNoneNoneN.A.
4928
340487412021
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exendin-4 39FreeAmidationLinearLNoneSalivary gland of the lizard Heloderma suspectumAntidiabetesBlood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h0.07 mg/kg0.32 ± 0.04Male SD rats plasma proteaseELISAMale SD rats plasmaIn VivoPDB id: 7MLLNoneEC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation)
4932
339400582021
gqsehhmrvysf
OPBP-112FreeFreeLinearDSubstituition of A with Y at position 10Derived from H12AnticancerCo-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h.8 mg/kg0.33 ± 0.01Male SD rats plasma proteaseRP-HPLCMale SD rats plasmaIn VivoNoneNoneAfter 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models.
4941
338254692021
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Native Ex439FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection.75 nmol/kg0.72 ± 0.07C57Bl/6 mice plasma proteaseFluorescence assayC57BL/6 mice plasmaIn VivoNoneNoneEC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency)
4953
338130912021
SGQYASHCWCWRDPGRSGGSK
FITC-TPP121FITC labelledFreeLinearLNoneSyntheticAnticancerBlood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding4 mg/kg<10 (Blood Clearance Half Life)Mice blood plasma proteaseFluorescence spectrometryMice blood plasmaIn VivoNoneNoneN.A.
4955
337918632021
DRVYIHP
125I-Ang1–77FreeFreeLinearL125I labeledSyntheticRole in Renal and Cardiovascular HomeostasisBlood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration4.5 mM0.6Rats plasma proteaseRadioactivity assayRats plasma In VivoNoneNoneAng1–7 exhibited 4.2±0.1%, 3.7±0.6%, 4.4±0.2%, and 2.6±0.4% binding capacity in D.D. water, PBS 50 mM, PBS10mM, and acetate bufer, respectively
4973
336563232021
PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFSQSIISTLT
IL-2132FreeFreeCyclic (C57-C104 Disulfide Bond)LNoneSyntheticAnticancer, Autoimmune diseases treatmentSerum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding0.6 mg/kg0.041 ± 0.006 (T1/2a )Mouse plasma proteaseSandwich ELISAMouse plasmaIn Vivopdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdfNoneKD (M) = (1.952 ± 0.130) × 10−8 for IL-2
4974
336563232021
PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFCQSIISTLT-(ED)6-LPETGGGK
B6146FreeLys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acidCyclic (C57-C104 Disulfide Bond) In IL-2LNoneSyntheticAnticancer, Autoimmune diseases treatmentSerum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding0.6 mg/kg0.613 ± 0.063(T1/2a )Mouse plasma proteaseSandwich ELISAMouse plasmaIn Vivopdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdfNoneKD (M) = (1.952 ± 0.130) × 10−8 for IL-2
4975
336563232021
PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFCQSIISTLT-(ED)6-LPETGGGK
B6 control146FreeLys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acidCyclic (C57-C104 Disulfide Bond) In IL-2LNoneSyntheticAnticancer, Autoimmune diseases treatmentSerum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding0.6 mg/kg0.035 ± 0.014(T1/2a )Mouse plasma proteaseSandwich ELISAMouse plasmaIn Vivopdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdfNoneKD (M) = (1.952 ± 0.130) × 10−8 for IL-2
4976
336563232021
PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFSQSIISTLT
IL-2132FreeFreeCyclic (C57-C104 Disulfide Bond)LNoneSyntheticAnticancer, Autoimmune diseases treatmentSerum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding0.6 mg/kg0.273 ± 0.040(T1/2b)Mouse plasma proteaseSandwich ELISAMouse plasmaIn Vivopdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdfNoneKD (M) = (1.952 ± 0.130) × 10−8 for IL-2
4978
336563232021
PTSSSTKKTQLQLEHLLLDLQMILNGINNYKNPKLTRMLTFKFYMPKKATELKHLQCLEEELKPLEEVLNLAQSKNFHLRPRDLISNINVIVLELKGSETTFMCEYADETATIVEFLNRWITFCQSIISTLT-(ED)6-LPETGGGK
B6 control146FreeLys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acidCyclic (C57-C104 Disulfide Bond) In IL-2LNoneSyntheticAnticancer, Autoimmune diseases treatmentSerum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding0.6 mg/kg0.196 ± 0.114(T1/2b)Mouse plasma proteaseSandwich ELISAMouse plasmaIn Vivopdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdfNoneKD (M) = (1.952 ± 0.130) × 10−8 for IL-2
4981
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic StrokePlasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion1 mg0.26 ± 0.02Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4982
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic StrokePlasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion4 mg 0.36 ± 0.04Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4983
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic StrokePlasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion10 mg0.45 ± 0.05Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4984
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic StrokePlasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion20 mg0.55 ± 0.07Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4985
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic StrokePlasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion30 mg0.70 ± 0.08Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4986
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic Strokeplasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion45 mg0.73 ± 0.05Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4987
336077002021
KEIVSRNKRRYQEDGRKKRRQRRR
Tat-K1324FreeFreeLinearLNoneSyntheticTreatment of Ischemic Strokeplasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion60 mg0.78 ± 0.06Human plasma protease UPLC–MS/MSHuman plasmaIn VivoNoneNoneN.A.
4989
336071652021
KKPYIL
JMV4386Both Arg residues in positions 1 and 2 were replaced by two LysFreeLinearLNoneDerived from NTAnalgesic without hypothermiaPlasma collected at 0, 1, 2, 5, 10, 30 and 60 min0.156 mM1.57 ± 0.27Rats plasma proteaseUPLC-MSRats plasma In VivoNoneNone(Binding) Ki (nM) = 4.00 ± 0.35 for hNTS1
4990
336071652021
KΨ[CH2NH]KPYIL
JMV4496FreeFreeLinearLArg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 Derived from NTAnalgesic without hypothermiaPlasma collected at 0, 1, 2, 5, 10, 30 and 60 min0.156 mM8.37 ± 2.02Rats plasma proteaseUPLC-MSRats plasma In VivoNoneNone(Binding) Ki (nM) = 2.02 ± 0.80 for hNTS1
5006
333875932021
CDLPQTHSLGSRRTLMLLAQMRKISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMKEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
Wild-type (IFN)165FreeFreeLinearLNoneHuman derivedAntiviral, AntiproliferativeBlood samples were taken at different times post-injection 100000 U0.9 ± 0.1 (T1/2 Elimination)Rats plasma proteaseSandwich ELISARats plasma In VivoPDB id: 1ITFNoneAntiviral SBA (IU/ng) = 201 ± 9 in wild-type IFN, Antiproliferative SBA (IU/ng) = 240 ± 50
5010
332459512021
YAEGTFISDYSIAMDKIRQQNFVNWLLAQKGKKSDWKHNITQ
GIP(1–42)42FreeFreeLinearLNoneSecreted by entero-endocrine K cells located in the proximal intestineInsulinotrophic EffectBlood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min and then co-incubation with Val-Pyr25 nmol/kg5 ± 0.6Mouse plasma proteaseRIAMouse plasmaIn Vivohttps://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type=NoneN.A.
5011
331354602021
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNoneProduced by the alpha cells of the pancreasAntidiabetes1 day0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) 4.01 ± 1.19Human male blood proteaseTwo site ELISA Human male blood sampleIn Vivopdb id: 1GCNNoneN.A.
5012
331354602021
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNoneProduced by the alpha cells of the pancreasAntidiabetes1 day0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) 3.94 ± 1.10Human female blood proteaseTwo site ELISA Human female blood sampleIn Vivopdb id: 1GCNNoneN.A.
5013
331354602021
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNoneProduced by the alpha cells of the pancreasAntidiabetes1 day0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) 3.96 ± 1.12Human blood protease (All)Two site ELISA Human blood sample (All)In Vivopdb id: 1GCNNoneN.A.
5014
331298372021
VDKPPYLPRPRPIRrPGGr
OM19r-819FreeAmidationLinearMixreplacing L-Arg15,19 with D-Arg15,19Derived from the antibacterial peptide OM19RAntibacterialBlood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min1 mg/ml1.632 ± 0.34 (Elimination Half Life)Wistar rats blood proteaseN.A.Wistar rats blood sampleIn VivoNoneNoneMIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin
5015
331298372021
VDKPPYLPRPRPIRrPGGr
mPEG5- OM19r-8 19mPEG5AmidationLinearMixreplacing L-Arg15,19 with D-Arg15,19Derived from the antibacterial peptide OM19RAntibacterialBlood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min1 mg/ml28.09 ± 2.81 (Elimination Half Life)Wistar rats blood proteaseN.A.Wistar rats blood sampleIn VivoNoneNoneMIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin
5042
320786722020
KTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELL
rFVIII654FreeFreeLinearLNoneSyntheticRole In ClottingN.A.150 IU/kg0.23DKO mice plasma proteasechromogenic activity assaysDKO mice plasmaIn VivoPDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdfNoneED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar
5057
332039162020
VRERGPQRVAAHITGTRGRSNTLSSPNSKNEKALGRKINSWESSRSGHSFLSNLHLRNGELVIHEKGFYYIYSQTYFRFQEEIKENTKNDKQMVQYIYKYTSYPDPILLMKSARNSCWSKDAEYGLYSIYQGGIFELKENDRIFVSVTNEHLIDMDHEASFFGAFLVG
Native TRAIL168FreeFreeLinearLNoneSyntheticAnticancerBlood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h0.01 mg/mL3.4 ± 1.1 BALB/c wild type mice plasma proteaseWestern blottingBALB/c wild type mice plasmaIn VivoPDB id: 1D0GNoneKD (M) = (6.02 ± 1.99) × 10–8 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.)
5058
332039162020
VRERGPQRVAAHITGTRGRSNTLSSPNSKNEKALGRKINSWESSRSGHSFLSNLHLRNGELVIHEKGFYYIYSQTYFRFQEEIKENTKNDKQMVQYIYKYTSYPDPILLMKSARNSCWSKDAEYGLYSIYQGGIFELKENDRIFVSVTNEHLIDMDHEASFFGAFLVG-GSGGGSG
TRAIL-ATNC168FreeTRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helixLinearLNoneSyntheticAnticancerBlood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h1 mg/mL56.1 ± 5.8BALB/c wild type mice plasma proteaseWestern blottingBALB/c wild type mice plasmaIn VivoPDB id: 1D0GNoneKD (M) = (2.56 ± 2.58) × 10–10 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.)
5059
332039162020
VRERGPQRVAAHITGTRGRSNTLSSPNSKNEKALGRKINSWESSRSGHSFLSNLHLRNGELVIHEKGFYYIYSQTYFRFQEEIKENTKNDKQMVQYIYKYTSYPDPILLMKSARNSCWSKDAEYGLYSIYQGGIFELKENDRIFVSVTNEHLIDMDHEASFFGAFLVG-GSGGGSG
TRAIL-ATNCIL4rP168FreeTRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helix followed by (MMP2) cleavage site (GPLGLAG) then IL4rP (CRKRLDRNC)LinearLNoneSyntheticAnticancerBlood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h1 mg/mL53.6 ± 5.8BALB/c wild type mice plasma proteaseWestern blottingBALB/c wild type mice plasmaIn VivoPDB id: 1D0GNoneIC50 value of 0.48 nM for TRAIL-ATNCIL4rP
5072
328880782020
QHSQITKV
Mouse Lau- PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.3Simulated intestinal fluid proteaseHPLCSimulated intestinal fluid In VitroNoneNoneN.A.
5075
328880782020
QHTQITKV
Human Lau-PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.650% W/V liver homogenate proteaseHPLC50% w/v liver homogenate In VitroNoneNoneN.A.
5076
328880782020
QHSQITKV
Mouse Lau- PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.9550% W/V liver homogenate proteaseHPLC50% w/v liver homogenate In VitroNoneNoneN.A.
5079
328880782020
QHTQITKV
Human Lau-PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.1550% V/V mouse plasma proteaseHPLC50% v/v mouse plasmaIn VitroNoneNoneN.A.
5081
328880782020
QHTQITKV 
Human Myr-PTEN-PDZ8N-myristoylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.1150% V/V Mouse Plasma ProteaseHPLC50% v/v Mouse plasmaIn VitroNoneNoneN.A.
5082
328880782020
QHSQITKV
Mouse Myr-PTEN-PDZ8N-myristoylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.8750% V/V Mouse Plasma ProteaseHPLC50% v/v Mouse plasmaIn VitroNoneNoneN.A.
5083
328880782020
QHTQITKV
Human Lau-PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.3650% W/V Brain Homogenate ProteaseHPLC50% w/v Brain HomogenateIn VitroNoneNoneN.A.
5084
328880782020
QHSQITKV
Mouse Lau- PTEN-PDZ8N-LaurylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.250% W/V Brain Homogenate ProteaseHPLC50% w/v Brain HomogenateIn VitroNoneNoneN.A.
5085
328880782020
QHTQITKV 
Human Myr-PTEN-PDZ8N-myristoylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.1650% W/V Brain Homogenate ProteaseHPLC50% w/v Brain HomogenateIn VitroNoneNoneN.A.
5086
328880782020
QHSQITKV
Mouse Myr-PTEN-PDZ8N-myristoylFreeLinearLLipidationSyntheticTreatment of Alzheimer's diseasesSamples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 minPeptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL)0.2550% W/V Brain Homogenate ProteaseHPLC50% w/v Brain HomogenateIn VitroNoneNoneN.A.
5087
328581242020
hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip
Cmpd# 316AcetylationFreeLinearMixhArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acidDerived from pyr-apelin-13Treatment of Chronic Hepatic FailureN.A.0.1 mg/kg0.362Male SD rats plasma proteaseScintillation proximity assayMale SD rats plasmaIn VivoNoneNoneRat GTPγS (nM) EC50 ± SE = 1.95 ± 1.16
5111
328122822020
SYSMEHFRWGKPVG
α-MSH14FreeFreeLinearLNoneDeriving from the pro-opimelanocortin (POMC)Stimulates The Production And Release Of Melanin By Melanocytes 4 ◦C for 15 min40 μM7.4Human plasma proteaseRP-HPLCHuman plasmaIn VitroNoneNoneN.A.
5114
328086592020
LRKHNCLQRRCMPLHSRVPFP
ELA-2121FreeFreeLinearLNoneproduced endogenously in the bodyAnti-Heart Failure ActivityBlood was collected at time points of 0, 3, 10, 30 and 90 mins, and 4.5, 12 and 24 h100 mg/kg∼13Mice plasma proteaseWestern blottingMice plasmaIn Vivohttps://sci-hub.se/10.1016/j.ijcard.2019.04.089NoneEC50 = 0.6 nM (cAMP supression)
5116
328030732020
GSLTSSERIDKQIRYILDGISALRKETCNKSNMCESSKEALAENNLNLPKMAEKDGCFQSGFNEETCLVKIITGLLEFEVYLEYLQNRFESSEEQARAVQMSTKVLIQFLQKKAKNLDAITTPDPTTNASLLTKLQAQNQWLQDMTTHLILRSFKEFLQSSLRALRQM
WT-Rb168FreeFreeLinearLBiotinylationSyntheticAntitumorBlood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h10 mg/kg20 (Initial Half-Life)Mice plasma proteaseSandwich ELISAMice plasmaIn VivoPDB ID: 4J4LNoneThe tumor size remained around 200 mm3 until 27 days when Pal-Rb was administered (p < 0.01), whereas tumor continued to grow over 600 mm3 when WT-Rb and PBS were injected.
5118
327593652020
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGR
hAβ4040FreeFreeLinearLNoneSynthesized in neurons and degraded in the brain and liverTreatment of Alzheimer's diseasesSerial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose68.5 ± 12.0 µg/kg16.8±5.66 (Terminal Half Life)(IP) corn oil treated rats plasma proteaseELISACorn oil treated rat plasmaIn Vivopdb id: 8KEWNoneN.A.
5119
327593652020
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGR
hAβ4040FreeFreeLinearLNoneSynthesized in neurons and degraded in the brain and liverTreatment of Alzheimer's diseasesSerial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose64.5 ± 13.2 µg/kg24.5±0.05 (Terminal Half Life)Untreated rats plasma proteaseELISAuntreated rats plasma In Vivopdb id: 8KEWNoneN.A.
5121
327593652020
MLPGLALLLLAAWTARALEVPTDGNAGLLAEPQIAMFCGR
hAβ4040FreeFreeLinearLNoneSynthesized in neurons and degraded in the brain and liverTreatment of Alzheimer's diseasesSerial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose68.5 ± 12.0 µg/kg47.9 ± 20.9 (Terminal Half Life)(IP) corn oil treated rats CSF proteaseELISACorn oil treated rat CSF In Vivopdb id: 8KEWNoneN.A.
5122
327362622020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
EX39FreeAmidationLinearLNoneProduced by the salivary glands of Gila monsterAntiobesityBlood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio50 nmol/kg0.69ICR mice plasma proteaseELISAICR mice plasmaIn VivoNoneNoneKd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1))
5128
326036662020
V
V-Gem1FreeGemicitabineLinearLNoneDerived from GemcitabineAnticancer2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min76 nmol/g46.2Mice blood plasma proteaseLC-MS/MSMice blood plasma (analyte = Gemcitabine)In VivoNoneNoneN.A.
5130
326036662020
V
V-Gem1FreeGemicitabineLinearLNoneDerived from GemcitabineAnticancer2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min76 nmol/g3.7Mice blood plasma proteaseLC-MS/MSMice blood plasma (analyte = Prodrug)In VivoNoneNoneN.A.
5131
326036662020
V
V-Gem1FreeGemicitabineLinearLNoneDerived from GemcitabineAnticancer2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min228 nmol/g39.1Mice blood plasma proteaseLC-MS/MSMice blood plasma (analyte = Gemcitabine)In VivoNoneNoneN.A.
5133
325826242020
RRPYIL
NT(8-13)6FreeFreeLinearLNoneDerived from NTImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM1.0 ± 0.1Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 1.5 ± 0.03 for hNTS1
5134
325826242020
KKPYIL
Entry 16KK amino acid substiuitionsFreeLinearLNoneNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM1.6 ± 0.3Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 4.0 ± 0.4 for hNTS1
5135
325826242020
Kψ(CH2NH)KPYIL 
Entry 26Kψ[CH2NH]K substiuition at position 1FreeLinearLNoneNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM8.4 ± 2.0Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 2.0 ± 0.8 for hNTS1
5136
325826242020
KKPYI
Entry 35KK amino acid substiuitionsTMSAla conjugationLinearLNoneNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM1.6 ± 0.3Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 0.018 ± 0.004 for hNTS1
5138
325826242020
KK-Sip-YIL
Entry 56KK amino acid substiuitionsFreeLinearLSip amino acid substiutionNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM4.5 ± 0.8Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 14 ± 11 for hNTS1
5140
325826242020
KK-Sip-YI
Entry 75Kψ[CH2NH]K substiuitionTMSAla conjugationLinearLSip amino acid substiution, TMSAla substuitionNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM3.5 ± 0.1Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 55 ± 5 for hNTS1
5142
325826242020
KKPKIL
Entry 96KK amino acid substiuitionsFreeLinearLSubstiution of Y amino acid with KNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM2.9 ± 0.2Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 7 600 ± 1 000 for hNTS1
5144
325826242020
KKPKI
Entry 115KK amino acid substiuitionsTMSAla-OH conjugationLinearLSubstiution of Y amino acid with KNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM2.8 ± 0.1Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 710 ± 100 for hNTS1
5146
325826242020
KKPwI
Entry 135KK amino acid substiuitionsTMSAla-OH conjugationLinearMixSubstiution of Y amino acid with d-WNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM10 ± 2 Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 3 600 ± 600 for hNTS1
5148
325826242020
KKP-Dmt-Tle-L
Entry 156KK amino acid substiuitionsFreeLinearLSubstiution of Y, I amino acid with Dmt, TleNT(8-13) analogsImprove Nts1-Induced Protective HypothermiaNT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C0.156 mM4.6 ± 0.6Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneBinding, Ki (nM) = 57 ± 6 for hNTS1
5150
325121812020
LEDGPKFL
[3H]-THF8FreeFreeLinearL3H labeling at proline5 residueIsolated from calf thymusAntiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min93 nmol/mL3.7 ± 0.2 Rats blood proteaseN.A.Rats blood sampleIn VitroNoneNoneN.A.
5151
325121812020
LEDGPKFL
[3H]-THF8FreeFreeLinearL3H labeling at proline5 residueIsolated from calf thymusAntiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min93 nmol/mL5.6 ± 0.2Mouse blood proteaseN.A.Mouse blood sampleIn VitroNoneNoneN.A.
5152
325121812020
LEDGPKFL
[3H]-THF8FreeFreeLinearL3H labeling at proline5 residueIsolated from calf thymusAntiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment)Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min93 nmol/mL5.2 ± 0.4Human blood protease N.A.Human blood sampleIn VitroNoneNoneN.A.
5153
325065012020
SYSMEHFRWGKPVG
des-Ac-a-MSH14FreeAmidationLinearLNoneDerived from POMCAntiinflammatory, Antipyretic37 °C2 µM0.21Human plasma proteaseGlo-sensor transfected cell-based luminescence assayHuman plasmaIn VitroNoneNoneEC50 (M) = 1.667E-09 for MC1R-des-Ac-a-MSH
5155
325065012020
YVMGHFRWDRFG
gamma2-MSH12FreeAmidationLinearLNoneDerived from POMCAntiobesity37 °C2 µM0.028Human plasma proteaseGlo-sensor transfected cell-based luminescence assayHuman plasmaIn VitroNoneNoneEC50 (M) = 7.749E-10 for MC1R-g2-MSH
5162
324045232020
WMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
C3434FreeFreeLinearLNoneDerived from the gp41 CHRTherapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus MonkeysBlood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h)1.7 μmol/kg0.6Rats plasma proteaseHIV inhibition assayRats plasmaIn VivoNoneNone[EC50] = 18.51 nM for PEG40-NC (antiviral activity)
5168
323481082020
Aib-EGTFTSDVSSYLEG-(Bis-pentenyl glycine)-AAKEFI-(S-octenyl alanine)-WLVKGR
SAH-GLP-1-A8J(23,30)28Aminoisobutyric acidFreeLinearLModifications include (S-octenyl alanine) and (Bis-pentenyl glycine)Single-stapled analogs of GLP-1Antidiabetes20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min 1 mM30Proteinase KLC-MS/MSDMSO + buffer consisting of 50 mM Tris HCl, pH 7.4In VitroPDB:3IOLNoneEC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5170
323481082020
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeFreeLinearLNoneUnstapled GLP-1 analogsAntidiabetes20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min 1 mM<10Proteinase KLC-MS/MSDMSO + buffer consisting of 50 mM Tris HCl, pH 7.4In VitroNoneNoneEC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5171
323481082020
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeFreeLinearLNoneUnstapled GLP-1 analogsAntidiabetes20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min 10 μM14Mouse plasma proteaseLC-MS/MSMouse plasmaIn VitroNoneNoneEC50 = 160 pM for SAH-GLP-1(16, 23, 30)
5174
323321432020
fQWAVGH
68Ga‐NeoBOMB1 768Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminalLinearLNoneSyntheticDOTA‐coupled GRPR‐antagonist2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i50 µg27.3Human plasma proteaseRP-HPLCHuman plasmaIn VivoNoneNoneN.A.
5175
323321432020
fQWAVGH
68Ga‐NeoBOMB1 768Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminalLinearLNoneSyntheticDOTA‐coupled GRPR‐antagonist2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i50 µg35Human blood proteaseRP-HPLCHuman blood sampleIn VivoNoneNoneN.A.
5182
322431372020
HsQGTFTSDYSKYLDSRRAQDFVQWLMNTKRNRNNIA
OXM-137FreeFreeLinearMixIncorporation of D-ser in place of L-ser at 2nd positionDerived from proglucagonAntiobesity, Antisteatotic N.A.40 μg/kg6 (Terminal Half Life)Mice plasma proteaseIn vitro cell based activity assayMice plasmaIn VivoNoneNoneEC50(nM) = 10 for OXM-1 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays)
5205
321333412020
RAAPYGVRLCGREFIRAVIFTCGGSRW
R3 B1-27 27FreeFreeLinearLNoneNative relaxin-3Roles in metabolism, arousal, learning and memoryN.A.0.05 μg/μl3.1Human serum proteaseLC-MSHuman serumIn VitroNoneNoneBinding affinity pKi ± SEM [logM] = 5.91 ± 0.21 
5206
321333412020
RAAPYGVRLSGREFIRAVIFTSR
R3 B1-22R23FreeAmidationLinearLNoneSyntheticRelaxin-3 antagonistN.A.0.05 μg/μl4Human serum proteaseLC-MSHuman serumIn VitroNoneNoneBinding affinity pKi ± SEM [logM] = 6.76 ± 0.03 
5213
320758702020
HADGSFSDEMNTILDNLAARDFINWLIQTKITD
hGLP-233FreeFreeLinearLNoneDerived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 6 h post injection1 mg/kg6.4 ± 0.2 (Elimination Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.07 for hGLP-2 receptor
5214
320758702020
FGEGTFSSELATILDALAARDFIAWLIATKITDKKKKKK
Glepaglutide39FreeKKKKKK amino acids substiuitions at C terminalLinearLG,E,T,S,L,A,A,A,A amino acid substuitions at positions 2,3,5,8,10,11,16,24,28 respectivelyDerived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 6 h post injection0.2 mg/kg19 ± 1.9 (Elimination Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.03 for hGLP-2 receptor
5215
320758702020
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLG amino acid substituition at position 2Derived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 6 h post injection0.2 mg/kg16 ± 0.8 (Elimination Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.09 for hGLP-2 receptor
5219
320758702020
HGDGSFSDE-Nle-fTILDLLAARDFINWLIQTKITD
Apraglutide33FreeAmidationLinearLGly2, Nle10, D-Phe11, Leu16 modification Derived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 6 h post injection0.100 mg/kg43 ± 4 (Elimination Half Life)Male cynomolgus monkeys plasma proteaseLC-MS/MSMale cynomolgus monkeysIn VivoNoneNoneEC50(nM) = 0.09 for hGLP-2 receptor
5223
320758702020
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLG amino acid substituition at position 2Derived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 169 h post injection1 mg/kg0.5 ± 0.1 (Terminal Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.09 for hGLP-2 receptor
5224
320758702020
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLG amino acid substituition at position 2Derived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 169 h post injection5 mg/kg0.5 ± 0.0 (Terminal Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.09 for hGLP-2 receptor
5227
320758702020
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
Teduglutide33FreeFreeLinearLG amino acid substituition at position 2Derived from hGLP-2Treatment of Short Bowel Syndrome Blood samples were collected at multiple time points up to 169 h post injection0.25 mg/kg0.9 ± 0.1 (Terminal Half Life)Male cynomolgus monkeys plasma proteaseLC-MS/MSMale cynomolgus monkeys plasmaIn VivoNoneNoneEC50(nM) = 0.09 for hGLP-2 receptor
5234
319267742020
QHWSYLLRP
Leuprolide10FreeNHEt (Ethylamine)LinearLNoneSyntheticAnticancer (Treatment of Advanced Prostate Cancer)Blood samples were collected from rats orbit at predetermined time interval1.0 mg/kg0.43 ± 0.025SD rats serum proteaseUPLC–MS/MSSD rats serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/NoneThe administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not
5235
319267742020
QHWSYLLRP
Leuprolide10FreeNHEt (Ethylamine)LinearLNone(GnRH) agonistAnticancer (Treatment of Advanced Prostate Cancer)Blood samples were collected from rats orbit at predetermined time interval1.0 mg/kg0.43 ± 0.06SD rats serum proteaseUPLC–MS/MSSD rats serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/NoneThe administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not
5236
319267742020
QHWSYLLRPX
PEG2K-LEU10FreeFreeLinearLPEGylation at His2Derived from leuprolideAnticancer (Treatment of Advanced Prostate Cancer)Blood samples were collected from rats orbit at predetermined time interval1.0 mg/kg0.53 ± 0.032SD rats serum proteaseUPLC–MS/MSSD rats serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/NoneThe weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group
5237
319267742020
QHWSYLLRPX
PEG2K-LEU10FreeFreeLinearLPEGylation at His2Derived from leuprolideAnticancer (Treatment of Advanced Prostate Cancer)Blood samples were collected from rats orbit at predetermined time interval1.0 mg/kg0.59 ± 0.023SD rats serum proteaseUPLC–MS/MSSD rats serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/NoneThe weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group
5241
318665652020
YSNSG 
YSNSG peptide5FreeFreeCyclicLNoneSyntheticAntitumorBlood samples from blood vessel in the tail were taken at the following time intervals: 15, 30, 60, 90 and 120 min20 mg/kg25.8 ± 8.2B16F1 melanoma mice plasma proteaseUPLC-MS/MSB16F1 melanoma mice plasmaIn VivoNoneNoneThe relative recoveries of the microdialysis probes of YSNSG peptide in mice using the reverse dialysis method were 79.3 ± 6.6% in the region 1 of the tumor and 79.1 ± 7.4% in the region 2 of the tumor
5255
315290972020
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
GH191FreeFreeLinearLNoneProduced by the somatotroph cells in the anterior pituitary glandInvolved in the regulation of growth and metabolismN.A.N.A.13.9 ± 3.6Human blood plasma protease2-site immunoassayHuman blood plasmaIn Vivopdb id: 1HWGNoneN.A.
5256
315290972020
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
GH191FreeFreeLinearLNoneProduced by the somatotroph cells in the anterior pituitary glandInvolved in the regulation of growth and metabolismN.A.N.A.17.0 ± 6.8Human blood plasma protease2-site immunoassayHuman blood plasma after SitagliptinIn Vivopdb id: 1HWGNoneN.A.
5257
315290972020
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
GH191FreeFreeLinearLNoneProduced by the somatotroph cells in the anterior pituitary glandInvolved in the regulation of growth and metabolismGH levels were obtained every 10 minutes from 8 PM until 8 AMN.A.13.9Human blood plasma protease2-site immunoassayHuman blood plasmaIn Vivopdb id: 1HWGNoneN.A.
5258
315290972020
FPTIPLSRLFDNAMLRAHRLHQLAFDTYQEFEEAYIPKEQKYSFLQNPQTSLCFSESIPTPSNREETQQKSNLELLRISLLLIQSWLEPVQFLRSVFANSLVYGASDSNVYDLLKDLEEGIQTLMGRLEDGSPRTGQIFKQTYSKFDTNSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF
GH191FreeFreeLinearLNoneProduced by the somatotroph cells in the anterior pituitary glandInvolved in the regulation of growth and metabolismGH levels were obtained every 10 minutes from 8 PM until 8 AMN.A.14.5Human blood plasma protease2-site immunoassayHuman blood plasma after 1month of SitagliptinIn Vivopdb id: 1HWGNoneN.A.
5259
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein10 mg/kg43 (T1/2, b)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5260
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein10 mg/kg9.9 (T1/2, a)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5261
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein5 mg/kg52 (T1/2, b)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5262
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein5 mg/kg12 (T1/2, a)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5263
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide39FreeAmidationLinearLGln28 modifcationsExenatide analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein10 mg/kg32 (T1/2, b)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5264
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide39FreeAmidationLinearLGln28 modifcationsExenatide analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein10 mg/kg8.3 (T1/2, a)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5265
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide39FreeAmidationLinearLGln28 modifcationsExenatide analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein5 mg/kg38 (T1/2, b)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5266
314799252020
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide39FreeAmidationLinearLGln28 modifcationsExenatide analogsAntidiabetesBlood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein5 mg/kg13 (T1/2, a)Cat plasma proteaseLC-MS/MSCat plasma (Diabetic)In VivoPDB id: 7MLLNoneN.A.
5274
N.A.2020
CSFPYRCLHQDLC
Ac-(06-34-18) Phe2 Tyr412AcetylationFreeLinearLTryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with TyrSyntheticTargets plasma kallikreinN.A.5 uM0.9Rats plasma proteaseWaters Xevo TQ-MSRats plasmaIn VitroNoneUS 201214350192 AIC50(nM)(rat kallikrein) = 13.8
5306
317746312019
HSDAVFDTNYTRLRKQVAAKKYLQSIKNKRY
BAY55-983731FreeFreeLinearLNoneSyntheticAntidiabetesN.A.5 mg/kg0.31Kunming mice plasma proteaseELISAKunming mice plasma In Vivohttps://sci-hub.se/10.2337/diabetes.51.5.1453NoneN.A.
5312
316323822019
Gu-ONNRPVYIPRPRPPHPRL
Api13718Gu: N,N,N',N' tetramethylguanidinoFreeLinearLO: L-ornithine at position 2Apidaecin analogAntimicrobialN.A.20 mg/kg< 30Mice plasma proteaseRP-HPLCMice plasmaIn VivoNoneNoneN.A.
5340
314432632019
RKDVY
TP5 5FreeFreeLinearLNoneArg32–Tyr36 fragment derived from thymopoietinAntiinflammatory (Treatment of Several Intestinal Inflammation Conditions)37 °CN.A.1.32 ± 0.24Rats plasma proteaesHPLC10 μg/mL rats plasmaIn VitroNoneNoneAmong the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL
5351
312774652019
CGFLG-C6-KTVRTSADE
Dox-peptide conjugate 1314DOXFreeCyclic (Lys6-Glu14 bond)LC6 fatty acid linked betweenSyntheticAnticancerSeveral aliquots (55 µL) were removed at 2, 5, 10, 15, 30, 60, 90, and 120 min125 µM11.8Human serum proteaseHPLC25% human serumIn VitroNoneNoneDox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25–35% as compared to Dox which reduced cell proliferation in the range of 20–34% for all selected four cell lines
5353
312760852019
RWVRWIOQVRpG
S-RWRWR peptide12AcetylationAmidationLinearMixR amino acid substituition at 1,4, 11, FAM denotes 5,6-carboxyfluorescein conjugated with Orn,p=D-Proline11,O=Ornithine7scrambled version of the RWRWR peptideCell penetrating peptide37°C2 mg/ml30HeLa lysates proteaseRP-HPLCHeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6)In VitroNoneNoneN.A.
5354
312760852019
GGAYAAPFKKKA
III-67B12FAM denotes 5,6-carboxyfluoresceinAmidationLinearLNoneSyntheticCell penetrating peptide37°C2 mg/ml9.5HeLa lysates proteaseRP-HPLCHeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6)In VitroNoneNoneN.A.
5355
312355322019
PGQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC
CNP-3939Proline substituition (amino acid 1) FreeCyclic (1 Disulfide Bond)LGlycine (amino acid 2) modifcationCNP derivativeTreatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal DysplasiasSamples from animals treated with the daily CNP-39 molecule were also obtained after the 1st and the 26th dose: at pre-dose, 0.08, 0.25, 0.5, 1, 2, and 4 hours postdose20 μg/kg per day for 26 weeks0.35Cynomolgus monkeys plasma proteasecompetitive radioimmunoassayCynomolgus monkeys plasmaIn VivoNoneNoneRatio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity)
5362
311945632019
CARSKNKDC
Fasudil in CAR-liposome 9Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal CysAmidationLinearLNoneSyntheticTreatment of Pulmonary Arterial Hypertension N.A.3 mg/kg0.7 ± 0.3 Sham rats plasma proteaseLC–MS/MSSham rats plasmaIn VivoNoneNoneN.A.
5370
311560412019
LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK
AD-114-Im7-FH 118Freelm7-FH fusionLinearLNoneFusion protein of AD-114 with lm7 and FHAttenuates Renal fibrosis through blockade Of CXCRBlood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing3 mg/kg0.18Mouse plasma proteaseLC–MS/MSMouse plasmaIn VivoPDB id: >5AEA_1NoneKd(nM) = 9.1 (Human CXCR4 affinity)
5371
311560412019
LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK
AD-114-Im7-FH-SA21 118Freelm7-FH-SA21LinearLNoneFusion protein of AD-114 with lm7 and FH, SA21Attenuates Renal fibrosis through blockade Of CXCRBlood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing2 mg/kg0.95Mouse plasma proteaseLC–MS/MSMouse plasmaIn VivoPDB id: >5AEA_1NoneKd(nM) = 9.2 (Human CXCR4 affinity)
5386
311008062019
MAATHEHSAQWLNNYKKGYGYGPYPLGINGGMHYGVDFFMNIGTPVKAISSGKIVEAGWSNYGGGNQIGLIENDGVHRQWYMHLSKYNVKVGDYVKAGQIIGWSGSTGYSTAPHLHFQRMVNSFSNSTAQDPMPFLKSAGYGKAGGTVTPTPNTGWKTNKYGTLYKSESASFTPNTDIITRTTGPFRSMPQSGVLKAGQTIHYDEVMKQDGHVWVGYTGNSGQRIYLPVRTWNKSTNTLGVLWGTIKLEHHHHHH
lysostaphin 255FreeFreeLinearLNoneProduced by Staphylococcus simulansAnti-Staphylococcal lysinBlood was collected by orbital bleeding at 1, 4, 7, and 24 h postadministration40 mg/kg<1Mice serum proteaseELISAMice serum In VivoNoneNoneUnconjugated lysostaphin shows a standard antibody binding response from 0.3 to 20 ng/ml.
5387
311008062019
MTCYYAGDFETTTNEEETEVWLSCFAKVIDYDKLDTFKVNTSLEDFLKSLYLDLDKTYTETGEDEFIIFFHNLKFDGSFLLSFFLNNDIECTYFINDMGVWYSITLEFPDFTLTFRDSLKILNFSIATMAGLFKMPIAKGTTPLLKHKPEVIKPEWIDYIHVDVAILARGIFAMYYEENFTKYTSASEALTEFKRIFRKSKRKFRDFFPILDEKVDDFCRKHIVGAGRLPTLKHRGRTLNQLIDIYDINSMYPATMLQNALPIGIPKRYKGKPKEIKEDHYYIYHIKADFDLKRGYLPTIQIKKKLDALRIGVRTSDYVTTSKNEVIDLYLTNFDLDLFLKHYDATIMYVETLEFQTESDLFDDYITTYRYKKENAQSPAEKQKAKIMLNSLYGKFGAKIISVKKLAYLDDKGILRFKNDDEEEVQPVYAPVALFVTSIARHFIISNAQENYDNFLYADTDSLHLFHSDSLVLDIDPSEFGKWAHEGRAVKAKYLRSKLYIEELIQEDGTTHLDVKGAGMTPEIKEKITFENFVIGATFEGKRASKQIKGGTLIYETTFKIRETDYLV
Cpl-1568FreeFreeLinearLNoneLytic enzyme of a pneumococcal bacteriophageAntimicrobial for Pneumococcal BacteremiaBlood was collected after 5, 10, and15 min from three animals and after 30, 60, and 120 min from the other three animals1.6 mg20.5Mice plasma proteaseWestern blotting and spot densitometryMice serumIn VivoNoneNoneMICs of Cpl-1 = 32 μg/ml
5388
311008062019
MEINVSKLRTDLPQVGVQPYRQVHAHSTGNPHSTVQNEADYHWRKDPELGFFSHIVGNGCIMQVGPVDNGAWDVGGGWNAETYAAVELIESHSTKEEFMTDYRLYIELLRNLADEAGLPKTLDTGSLAGIKTHEYCTNNQPNNHSDHVDPYPYLAKWGISREQFKHDIENGLTIETGWQKNDTGYWYVHSDGSYPKDKFEKINGTWYYFDSSGYMLADRWRKHTDGNWYWFDNSGEMATGWKKIADKWYYFNEEGAMKTGWVKYKDTWYYLDAKEGAMVSNAFIQSADGTGWYYLKPDGTLADRPEFTVEPDGLITVK
LytA318FreeFreeLinearLNoneDerived from Streptococcus pneumoniaeTherapeutic agent in experimental peritonitis sepsis caused by highly Β-lactam resistant Streptococcus PneumoniaeBlood samples were obtained from three animals per group, which were killed at 5, 15, 60, and 120 min3.1 mg/ml22.5Adult swiss mice plasma proteaseN.A.Adult swiss mice plasmaIn VivoNoneNoneMICs of LytA = 16 μg/ml 
5401
310693812019
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Tozuleristide36FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage)LFluorophore indocyanine green (ICG) at Lysine27Derived from chlorotoxin Used for fluorescence imaging of tozuleristide in adult subjects with gliomasCollected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery3 mg0.242Human serum proteaseLC-MS/MSHuman serumIn VivoPubChem id: 121488172NoneN.A.
5402
310693812019
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Tozuleristide36FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage)LFluorophore indocyanine green (ICG) at Lysine27Derived from chlorotoxin Used for fluorescence imaging of tozuleristide in adult subjects with gliomasCollected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery9 mg0.326Human serum proteaseLC-MS/MSHuman serumIn VivoPubChem id: 121488172NoneN.A.
5403
310693812019
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Tozuleristide36FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage)LFluorophore indocyanine green (ICG) at Lysine27Derived from chlorotoxin Used for fluorescence imaging of tozuleristide in adult subjects with gliomasCollected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery18 mg0.392Human serum proteaseLC-MS/MSHuman serumIn VivoPubChem id: 121488172NoneN.A.
5404
310693812019
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Tozuleristide36FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage)LFluorophore indocyanine green (ICG) at Lysine27Derived from chlorotoxin Used for fluorescence imaging of tozuleristide in adult subjects with gliomasCollected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery24 mg0.521Human serum proteaseLC-MS/MSHuman serumIn VivoPubChem id: 121488172NoneN.A.
5405
310693812019
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Tozuleristide36FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage)LFluorophore indocyanine green (ICG) at Lysine27Derived from chlorotoxin Used for fluorescence imaging of tozuleristide in adult subjects with gliomasCollected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery30 mg0.485Human serum proteaseLC-MS/MSHuman serumIn VivoPubChem id: 121488172NoneN.A.
5410
310641532019
KPA
Lys(Har)-PA3Side chain of the Lys residue in the first position was extended by attaching additional homoarginine (Har)FreeLinearLNoneKPPR analogsPeptidic inhibitor of the VEGF165/NRP-1 interaction100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h)1.1 µmol/mL39Human plasma proteaseHPLC-MS/MSHuman plasmaIn VitroNoneNoneIC50 = 0.2μM
5411
310641532019
Dab-R
Dab-R2Dab (2,4-diaminobutyric acid) substiuition at 1st positionFreeLinearLNoneKPPR analogsPeptidic inhibitor of the VEGF165/NRP-1 interaction100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h)1.1 µmol/mL44Human plasma proteaseHPLC-MS/MSHuman plasmaIn VitroNoneNoneIC50 = 0.3 μM
5414
310389302019
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneSyntheticAntidiabetesBlood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration25 nmol/kg0.9Mice plasma proteaseELISAMice plasmaIn VivoPDB id: 7MLLNoneExenatide presented similar GLP-1 activities with EC50 values of 1.1
5418
309863422019
NLLMAAS
T4-Cy5.57FreeConjugated with Cy5.5LinearLNoneSyntheticAntitumorN.A.N.A.1Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneFree T4 or P-T4 slowed tumor regrowth after chemotherapy, whereas the P-T4 treatment group exhibited a better suppressive effect
5423
309730072019
QNSPNIFGQWM
GBAP11FreeFreeCyclic (Ser3-Met11 bond)LNoneProduced by Enterococcus faecalisAntibacterialTime points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr0.28 mM<30Human plasma proteaseHPLCHuman plasmaIn VitroNoneNoneEC50 (nM) = 1.15 for GBAP
5424
309730072019
QNSPNI-NMeF-GQWM
GBAP 1114FreeFreeCyclic (Ser3-Met11 bond)LN-methylation at Phe7GBAP analogsAntibacterialTime points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr0.28 mM<30Human plasma proteaseHPLCHuman plasmaIn VitroNoneNoneEC50(nM) = 6.3 for GBAP-[N-MeF7]
5432
309019672019
EMTWEEWEKKIEEYTKKIEEILKKSQNQQIDL
HP23-E6-IDL32FreeFreeLinearLNoneSyntheticAntiviral (Anti-Hiv Activity)Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides HP23-E6-IDL5 mg/kg 1Mice serum proteaseN.A.Mice serum In VivoNoneNoneIC50(pM) = 912 ± 29 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of HP23-E6-IDL against infection by HIV-1 mutants resistant to T20)
5433
309003902019
SDKP
Ac-SDKP4Acetylation FreeLinearLNoneSyntheticAntifibrotic effects on Hepatic FibrosisAt 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein1 mg/kg9.65 ± 1.78 Rats serum proteaseRP-HPLCRats serumIn VivoNoneNoneAc-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5435
309003902019
SDKP
Ac-SDKP4Acetylation FreeLinearLNonesyntheticAntifibrotic Effects On Hepatic Fibrosis9 h at 37 C100 μM6.47 ± 1.53Human Serum ProteaseHPLChuman serumIn VitroNoneNoneAc-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro
5438
308170592019
EAENPQAGAVELGGGLGGLQALALEGPPQ
Porcine C‐Peptide29FreeFreeLinearLNoneReleased from the pancreatic beta cells when proinsulin is processed into insulin and C-peptideUsed as marker of insulin productionBlood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes 200 pmol/kg4.3 ± 1.2 (Terminal Elimination Half Life)Rats plasma proteaseELISARats plasmaIn Vivohttps://www.jbc.org/article/S0021-9258(19)41064-8/pdfNoneN.A.
5440
308170592019
EAENPQAGAVELGGGLGGLQALALEGPPQ
Porcine C‐Peptide29FreeFreeLinearLNoneReleased from the pancreatic beta cells when proinsulin is processed into insulin and C-peptideUsed as marker of insulin productionBlood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes 2000 pmol/kg6.9 ± 2.5 (Terminal Elimination Half Life)Rats plasma proteaseELISARats plasmaIn Vivohttps://www.jbc.org/article/S0021-9258(19)41064-8/pdfNoneN.A.
5441
308170592019
EAENPQAGAVELGGGLGGLQALALEGPPQ
Porcine C‐Peptide29FreeFreeLinearLNoneReleased from the pancreatic beta cells when proinsulin is processed into insulin and C-peptideUsed as marker of insulin productionBlood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection2000 pmol/kg53 ± 14 (Terminal Elimination Half Life)Rats plasma proteaseELISARats plasmaIn Vivohttps://www.jbc.org/article/S0021-9258(19)41064-8/pdfNoneN.A.
5442
308146522019
ASPAAPAPASPAAPAPSAPA
Adnectin C 20FreeFreeLinearLNoneDerived from the tenth domain of fibronectin type III (10thFn3)AnticancerBlood samples were taken after 5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, and 96 h5 mg/kg49.41Mice plasma proteaseELISAMice plasmaIn VivoNoneNoneKd(1/s) = 5.643E − 5 
5446
307946542019
GLSKGCFGLKLDRIGSMSGLGC
CNP(1–22) 22FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneCNP C terminal cleavageImproved endochondral ossification and accelerated bone growth in miceN.A.20 nmol/kg1.42 ± 0.45Rats plasma proteaseELISARats plasmaIn VivoNoneNoneN.A.
5447
307946542019
GLSKGCFGLKLDRIGSMSGLGCVQQRKDSKKPPAKLQPR
ASB2012339FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneC-type natriuretic peptide derivativeTreatment of Growth failure and DwarfismN.A.20 nmol/kg31.3 ± 4.8 Rats plasma proteaseELISARats plasmaIn VivoNoneNoneN.A.
5448
307946542019
GLSKGCFGLKLDRIGSMSGLGC
CNP(1–22) 22FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneCNP C terminal cleavageImproved Endochondral Ossification And Accelerated Bone Growth In MiceN.A.50 nmol/kg10.0 ± 5.0Rats plasma proteaseELISARats plasmaIn VivoNoneNoneN.A.
5449
307946542019
GLSKGCFGLKLDRIGSMSGLGCVQQRKDSKKPPAKLQPR
ASB2012339FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneC-type natriuretic peptide derivativeTreatment Of Growth Failure And DwarfismN.A.50 nmol/kg32.1Rats plasma proteaseELISARats plasmaIn VivoNoneNoneN.A.
5450
307564832019
GLAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALP
ABD–Dox47FreeDox conjugationLinearLNoneDerived from streptococcal protein GAnticancerBlood samples were collected at 40 s, 15 and 30 min, and 2, 4, 8, 24, 48, 72, and 96 h post injection 5 mg/kg29.4 ± 0.8 (Elimination Half Life)Mice plasma proteaseFlurorescence assayMice plasmaIn VivoNoneNone(IC50) of ABD–Dox was 6.4 × 10−6 for C26 cell
5452
307421452019
MAQAKHKQRKRLKSSCKRHPLYVDFSDVGWNDWIVAPPGYHAFYCHGECPFPLADHLNSTNHAIVQTLVNSVNSKIPKACCVPTELSAISMLYLDENEKVVLKNYQDMVVEGCGCR
Native BMP-2116FreeFreeLinearLNoneSyntheticPromotes Bone repairN.A.0.5 mg/kg<30N.A.Fluorescence spectrometryRatsIn VivoPDB id: 1ES7Nonen(BMP-2) did not enhance ALP expression in MSCs compared with native BMP-2 unless pretreated with IV collagenase, which significantly enhanced ALP expression and calcium deposition​
5453
307098672019
DRVYIHS
PNA57FreeReplaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminusLinearLNoneAng-(1-7) analogsTreating Vascular Cognitive Impairment and Inflammation related Memory DysfunctionN.A.100 µM1.0 ± 0.2 Rats serum proteaseTandem mass spectrometry (MS)Rats serumIn VitroNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5454
307098672019
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAng-(1-7) Decrease Brain ROS production and Inflammation in Preclinical models of HFN.A.100 µM0.25 ± 0.05Rats serum proteaseTandem mass spectrometry (MS)Rats serumIn VitroNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5455
307098672019
DRVYIHS
PNA57FreeReplaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminusLinearLNoneAng-(1-7) analogsTreating Vascular Cognitive Impairment and Inflammation related Memory DysfunctionN.A.10 mg/kg18.2 ± 3 Rats serum proteaseLC-MSRats serumIn VivoNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5456
307098672019
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAng-(1-7) Decrease Brain ROS production and Inflammation in Preclinical models of HFN.A.10 mg/kg20.9 ± 0.7Rats serum proteaseLC-MSRats serumIn VivoNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5457
307098672019
DRVYIHS
PNA57FreeReplaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminusLinearLNoneAng-(1-7) analogsTreating Vascular Cognitive Impairment and Inflammation related Memory DysfunctionN.A.10 mg/kg26.6 ± 3.6CSF proteaseLC-MSCSFIn VivoNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5458
307098672019
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAng-(1-7) Decrease Brain ROS production and Inflammation in Preclinical models of HFN.A.10 mg/kg24.7 ± 5CSF proteaseLC-MSCSFIn VivoNoneNonePotency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) 
5459
306904062019
KFRRQRPRLSHKGPMPF
Apelin1 17FreeFreeLinearLNoneNative apelin 17Blood Pressure lowering agents37 C for up to 72 hN.A.0.4RHNEPLC-MSApelin1 In VitroNoneNoneEC50(nM) = 1.9 ± 1.0
5460
306904062019
KFRKFRRQRPRLSHKGPMPF
Apelin220R1 = NH2-Lys-Phe-ArgFreeLinearLR2=HApelin analogsBlood Pressure lowering agents37 C for up to 72 hN.A.1RHNEPLC-MSApelin2In VitroNoneNoneEC50(nM) = 4.1 ± 1.0
5468
306904062019
KFRRQRPRLSHKGPMPF
Apelin1 17FreeFreeLinearLNoneNative apelin 17Blood Pressure lowering agents37 C for up to 72 hN.A.0.4RhKLKB1LC-MSApelin1 In VitroNoneNoneEC50(nM) = 1.9 ± 1.0
5469
306904062019
KFRKFRRQRPRLSHKGPMPF
Apelin220R1 = NH2-Lys-Phe-ArgFreeLinearLR2=HApelin analogsBlood Pressure lowering agents37 C for up to 72 hN.A.0.7RhKLKB1LC-MSApelin2In VitroNoneNoneEC50(nM) = 4.1 ± 1.0
5470
306904062019
KFRKFRRQRPRLSHKGPMPF
Apelin320R1 = NH2-Lys-Phe-ArgFreeLinearLR2=Me, Methylation at Glu8Apelin analogsBlood Pressure lowering agents37 C for up to 72 hN.A.0.9RhKLKB1LC-MSApelin3In VitroNoneNoneEC50(nM) = 4.9 ± 1.0
5473
306904062019
KFRKFRRQRPRLSHKGPMPF
Apelin620R1 = PALM-Lys-Phe-ArgFreeLinearLNoneApelin analogsBlood Pressure lowering agents37 C for up to 72 hN.A.1RhKLKB1LC-MSApelin6In VitroNoneNoneEC50(nM) = 2.6 ± 0.8
5477
306904062019
KFRRQRPRLSHKGPMPF
Apelin1 17FreeFreeLinearLNoneNative apelin 17Blood Pressure lowering agents37 C for up to 72 hN.A.0.02hplasma proteaseLC-MShplasmaIn VitroNoneNoneEC50(nM) = 1.9 ± 1.0
5478
306904062019
KFRKFRRQRPRLSHKGPMPF
Apelin220R1 = NH2-Lys-Phe-ArgFreeLinearLR2=HApelin analogsBlood Pressure lowering agents37 C for up to 72 hN.A.0.3hplasma proteaseLC-MShplasmaIn VitroNoneNoneEC50(nM) = 4.1 ± 1.0
5512
306067212019
CYNEFGCEDFYDIC
BCY-B214AcetylationFreeCyclic (Cyclized With 1,3,5-Trismethylbenzene On C1, C7, C14)LNoneBicyclic peptide derivativeFor imaging and targeting of proteins overexpressed by tumorsBlood samples were taken from two animals per time-point, at 0.08, 0.5, 1, 2, and 4 hours post injection (p.i.),5.925 mg/kg14 (Elimination Half Life)Mouse plasma proteaseLC-MS/MSMouse plasmaIn VivoNoneNoneKD(nM) = 25 ± 0.3
5513
306056342019
pGlu-RPRLSHKGPMPF
(Pyr)1-apelin-1313pGlu = PyroglutamateFreeLinearLNoneApelin analogsHemodynamic Effects In HumansN.A.50 mg/kg13Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneN.A.
5514
306056342019
pGlu-RPRLSHKGPMPF
(Pyr)1-apelin-1313pGlu = PyroglutamateFreeLinearLNoneApelin analogsHemodynamic Effects In HumansN.A.50 mg/kg16Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneN.A.
5520
305434202019
(QLYSALANKCCHVGVOKRSLARFC)-DSWMEEVIKLCGRELVRAQIAICGMSTWS
R253FreeFreeLinearLB-D1A Cys mutationR3 based relaxin analogsRole in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound HealingN.A.0.3 mg/kg0.3Mouse plasma proteaseLC-MSMouse plasmaIn VivoNoneNoneEC50(nM) = 0.025 ± 0.004 
5523
305434202019
(QLYSALANKCCHVGVOKRSLARFC)-(ASWMEEVIKLCGRELVRAQIAICGMSTWC)
R3-0253FreeFA-02LinearLB-S29C,D1A Cys mutationR3 based relaxin analogsRole in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound HealingN.A.0.3 mg/kg1Mouse plasma proteaseLC-MSMouse plasmaIn VivoNoneNoneEC50(nM) = 0.028 ± 0.18
5524
305434202019
(QLYSALANKCCHVGVOKRSLARFC)-(ASWMEEVIKLCGRELVRAQIAICGMSTWC)
R3-0253FreeFA-02LinearLB-S29C,D1A Cys mutationR3 based relaxin analogsRole In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound HealingN.A.0.3 mg/kg1Mouse plasma proteaseLC-MSmouse plasmaIn VivoNoneNoneEC50(nM) = 0.028 ± 0.10
5550
303341712019
CDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE
rhIFN-α2b165FreeFreeLinearLNoneSyntheticAntiviral, Antitumor, And Immunomodulatory EffectsN.A.500 μg/kg0.54 (Elimination Half Life)Rats plasma proteasesandwich ELISARats plasmaIn VivoPDB id: 1RH2NonerhIFN-α2b had a high specific antiviral activity (2.5 × 108 ± 1.1 × 108IU/mg protein)
5651
301759192018
GRP-MeArg-AFTF-MeAla-CKKK
Myristoylated peptide146FAM labelledAdditional C terminal cysteine linked to peptide using dislufide bondLinearLMeAla, MeArg,Lys1 modified with MyrSyntheticSubstrate reporter for PKBRT1 µM12 ± 1N.A.N.A.Axenic D. discoideum K-AX3 DB or SorCM after myristoylated peptide loadingIn VitroNoneNoneN.A.
5652
301759192018
GRP-MeArg-AFTF-MeAla
Electroporation peptide96FAM labelledFreeLinearLMeAla, MeArgSyntheticSubstrate reporter for PKBRT35 µM53 ± 15N.A.N.A.Axenic D. discoideum K-AX3 SorCM buffer after electroporationIn VitroNoneNoneN.A.
5653
301759192018
GRP-MeArg-AFTF-MeAla
Pinocystosis peptide96FAM labelledFreeLinearLMeAla, MeArgSyntheticSubstrate reporter for PKBRT150 µM19 ± 2N.A.N.A.Axenic D. discoideum K-AX3 DB after pinocytosisIn VitroNoneNoneN.A.
5658
301610022018
LLTHTISRIAVSYQTKVNLL
P1621FreeFreeLinearLNoneTNF-a cleaved fragmentAntitumorOrbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h)5 mg/kg0.07BALB/c mice plasma proteaseLC-MSBALB/c mice plasmaIn VivoNoneNoneN.A.
5659
301610022018
SVRSSSRTPSDKPVAHVVANPQAEGQLQWLNRRANALLANGVELRDNQLVVPSEGLYLIYSQVLFKGQGCPSTHVLLTHTISRIAVSYQTKVNLLSAIKSPCQRETPEGAEAKPWYEPIYLGGVFQLEKGDRLSAEINRPDYLDFAESGQVYFGIIAL
TNF-a158FreeFreeLinearLNoneTNF-aAntitumorOrbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h)5 mg/kg0.43BALB/c mice plasma proteaseLC-MSBALB/c mice plasmaIn VivoPDB id: 6OP0NoneN.A.
5664
300411532018
GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT
HI51FreeFreeCyclic (3 S-S Bond)LNoneSyntheticAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture1 µM<0.5Rats SCT proteaseLC-HRMS1 mg/ml rats SCT protein In Vitrohttps://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1NoneN.A.
5665
300411532018
GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT
HI51FreeFreeCyclic (3 S-S Bond)LNoneSyntheticAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture1 µM<0.5Rats SCT proteaseLC-HRMS2 mg/ml rats SCT protein In Vitrohttps://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1NoneN.A.
5666
300411532018
GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT
HI51FreeFreeCyclic (3 S-S Bond)LNoneSyntheticAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture1 µM<0.5Rats SCT proteaseLC-HRMS4 mg/ml rats SCT protein In Vitrohttps://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1NoneN.A.
5669
300411532018
GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT
HI51FreeFreeCyclic (3 S-S Bond)LNoneSyntheticAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture10 µM0.56Rats SCT proteaseLC-HRMS4 mg/ml rats SCT protein In Vitrohttps://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1NoneN.A.
5674
300411532018
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK
Lixisenatide 44FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture10 µM<0.5Human SCT proteaseLC-HRMS1 mg/ml human SCT proteinIn VitroNoneNoneN.A.
5678
300411532018
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK
Lixisenatide 44FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture10 µM<0.5SD rats SCT proteaseLC-HRMS1 mg/ml SD rats SCT proteinIn VitroNoneNoneN.A.
5680
300411532018
H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVRGRG
Semaglutide31FreeFreeLinearLAib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18)GLP-1 analogsAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture10 µM0.9SD rats SCT proteaseLC-HRMS1 mg/ml SD rats SCT proteinIn VitroNoneNoneN.A.
5682
300411532018
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK
Lixisenatide 44FreeAmidationLinearLNoneGLP-1 analogsAntidiabetesAt each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture10 µM<0.5Göttingen minipigs SCT proteaseLC-HRMS1 mg/ml göttingen minipigs SCT proteinIn VitroNoneNoneN.A.
5697
299586972018
TLQPPASSRRRHFHHALPPAR
125I-TLQP-2121125I labelledFreeLinearLNoneDerived from the proteolytic cleavage of the 617-aa VGFIsoproterenol stimulated lipolysisAt the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL)1 mM1.7 (T1/2 Initial Phase)Rats plasma proteaseLC-MS Rats plasma In VitroNoneNoneN.A.
5725
297525652018
YGGFM
Met-enkephalin5FreeMet substituition at C terminalLinearLNoneSyntheticInvolved in the pain modulating mechanism in the spinal cordIncubated over 0, 30, 60, 90, 120 min at 37 °C0.0413 mM27 ± 1NEP (5.687 Nm)RP-HPLCTris–HCl buffer (50 mM, pH 7.4)In VitroNoneNoneN.A.
5728
297525652018
YGGFM
Met-enkephalin5FreeMet substituition at C terminalLinearLNoneSyntheticInvolved in the pain modulating mechanism in the spinal cordIncubated over 0, 30, 60, 90, 120 min at 37 °C0.0413 mM47 ± 1NEP (5.687 Nm)RP-HPLCTris HCl buffer with 0.156 mM [Ala1]sialorphin inhibitor In VitroNoneNoneN.A.
5731
297525652018
YGGFM
Met-enkephalin5FreeMet substituition at C terminalLinearLNoneSyntheticInvolved in the pain modulating mechanism in the spinal cordIncubated over 0, 30, 60, 90, 120 min at 37 °C0.0413 mM42 ± 2NEP (5.687 Nm)RP-HPLCTris HCl buffer with 0.156 mM[Ala4]sialorphin inhibitor In VitroNoneNoneN.A.
5732
297525652018
YGGFM
Met-enkephalin5FreeMet substituition at C terminalLinearLNoneSyntheticInvolved in the pain modulating mechanism in the spinal cordIncubated over 0, 30, 60, 90, 120 min at 37 °C0.0413 mM52 ± 2NEP (5.687 Nm)RP-HPLCTris HCl buffer with 0.156 mM [Ala5]sialorphin inhibitor In VitroNoneNoneN.A.
5734
297525652018
YGGFM
Met-enkephalin5FreeMet substituition at C terminalLinearLNoneSyntheticInvolved in the pain modulating mechanism in the spinal cordIncubated over 0, 30, 60, 90, 120 min at 37 °C0.0413 mM53 ± 1NEP (5.687 Nm)RP-HPLCTris HCl buffer with 0.156 mM [Ser4]sialorphin inhibitor In VitroNoneNoneN.A.
5744
297210652018
WHSDMEWWYLLG
64Cu-DOTA-F561264Cu-DOTAFreeLinearLNoneSyntheticAntiangiogenic At 10, 30, 60, and 120 min7.4 mBq0.4249Mice plasma proteaseRadioactivity assayMice plasmaIn VivoNoneNoneF56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way
5749
296850372018
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAng-(1-7) Decrease brain ROS production and inflammation in preclinical models of HF15 h at 37°C100 µM13.8 ± 5.7Rats serum proteaseHPLCRats serumIn VitroNoneNoneAng-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5752
296850372018
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAng-(1-7) Decrease brain ROS production and inflammation in preclinical models of HFAfter a 30 min incubation at 37°C0.1 mM9.2 ± 0.5ACE, LAP and NEPHPLCPBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEPIn VitroNoneNoneAng-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice
5762
296698112018
MKYLLPTAAAGLLLLAAQPAMAAHHHHHHGSSGGGENLYFQGSSGQVQLVQSGAEVKKPGASVKVSCKASGYTFTDHAIHWVRQAPGQRLEWMGYFSPGNDDFKYSQKFQGRVTITADKSSSTAYMELSSLRSEDTAVYYCARSWIMQYWGQGTLVTVSSGGGGSDIVMTQSPDSLAVSLGERATINCKSSQSVLYSSNNKNYLAWYQQKPGQPPKLLIYWASTRESGVPDRFSGSGSGTDFTLTISSLQAEDVAVYYCQQYYSYPLTFGGGTKVEIK
125I-3E8.G4S278125I labelledFreeLinearL125I-labeled, VH and VL joined by G4S linkerDerived from the 3E8 antibodyOptimizes biophysical properties, serum half-life and high-specificity tumor imagingBlood samples (5 μl) were drawn from the saphenous vein by puncture, using a 30-gauge syringe needle, at 0.5, 1, 5, 24, 48, and 72 h postinjection for 3E8.G4S5 μCi0.67Mice blood proteaseRadioiodination assayMice blood sampleIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/instance/5995523/bin/supp_RA118.002538_136163_1_supp_109995_p6kvvq.pdfNoneKD of 3.6 nM for 3E8.G4S
5766
296564722018
KVTAMTCFLL
[K6T]P8 peptide10FreeAmidationLinearLK6T modificationSyntheticIL‐15 antagonist peptideAt t = 0, 5, 8, 10, 20,30, 45, 60, 90, and 120 minutes100 μM.5.88 ± 1.73Human synovial fluids proteaseRP-HPLCHuman synovial fluidsIn VitroNoneNoneIC50 values of 27.7 μM
5773
296023082018
HSTPSSP
P4-Chlorambucil7FreeChlorambucilLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 21.5N.A.LC–MS/MSBuffer pH 7.4In VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5774
296023082018
HSTPSSP
P4-Chlorambucil7FreeChlorambucilLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 12.4Mouse liver homogenate proteaseBCA protein assayMouse liver homogenateIn VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5775
296023082018
HSTPSSP
P4-Melphalan7FreeMelphalanLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 24.6N.A.LC–MS/MSBuffer pH 7.4In VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5776
296023082018
HSTPSSP
P4-Melphalan7FreeMelphalanLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 10.6Mouse liver homogenate proteaseBCA protein assayMouse liver homogenateIn VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5777
296023082018
HSTPSSP
P4-Bendamustine7FreeBendamustineLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 19.3N.A.LC–MS/MSBuffer pH 7.4In VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5778
296023082018
HSTPSSP
P4-Bendamustine7FreeBendamustineLinearLNoneProtein drug conjugateAnticancer37 °C100 μl/ ml 15.4Mouse liver homogenate proteaseBCA protein assayMouse liver homogenateIn VitroNoneNoneThe efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM
5786
295500182018
MSDKPDMAEIEKFDKSKLKKTETQEKNPLPSKETIEQEKQAGESGSMSDKPDMAEIEKFDKSKLKKTETQEKNPLPSKETIEQEKQAGES
DTβ4 88FreeFreeLinearLDimerization using GS linkerDimeric Tβ4Protects post-ischemic cardiac functionN.A.50 μg59.1Mouse serum proteaseHPLCMouse serumIn VivoUniprot id: P62328NoneIn scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration 
5787
295500182018
MSDKPDMAEIEKFDKSKLKKTETQEKNPLPSKETIEQEKQAGES
Tβ443FreeFreeLinearLNoneSyntheticProtects post-ischemic cardiac functionN.A.50 μg53.3Mouse serum proteaseHPLCMouse serumIn VivoUniprot id: P62328NoneIn scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration 
5788
295403152018
HGDGSFTSELSTYLDALAARDFIAWLIQTKITD
GUB09-123 33FreeAmidationLinearLNoneSyntheticGLP-1/GLP-2 co-agonistBlood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point)800nmol/kg0.9Mice plasma proteaseLC-MS/MSMice plasmaIn VivoNoneNoneGLP-1R, EC50 (nM) = 0.07
5794
295318582018
KCRGDCFC
[68Ga]Ga-DOTA-RGD8CH2CO chemical group attached, DOTA conjugated with Lys1CCPEGCyclic (C2-C6 Disulfide Bond)L68Ga labellingSyntheticPET imaging agent to visualize and quantify angiogenesisBlood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injectionN.A.24.6 (Slow Phase)NHP plasma proteaseUV-HPLC and LC-ESI-MSNHP uterus plasma without NC-100717N.A.NoneNoneN.A.
5795
295318582018
KCRGDCFC
[68Ga]Ga-DOTA-RGD8CH2CO chemical group attached, DOTA conjugated with Lys1CCPEGCyclic (C2-C6 Disulfide Bond)L68Ga labellingSyntheticPET imaging agent to visualize and quantify angiogenesisBlood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injectionN.A.1.1 (Fast Phase)NHP plasma proteaseUV-HPLC and LC-ESI-MSNHP uterus plasma without NC-100717N.A.NoneNoneN.A.
5796
295318582018
KCRGDCFC
[68Ga]Ga-DOTA-RGD8CH2CO chemical group attached, DOTA conjugated with Lys1CCPEGCyclic (C2-C6 Disulfide Bond)L68Ga labellingSyntheticPET imaging agent to visualize and quantify angiogenesisBlood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection1 mg/kg26.4 (Slow Phase)NHP plasma proteaseUV-HPLC and LC-ESI-MSNHP uterus plasma after administration of NC-100717 (1 mg/kg)In VivoNoneNoneN.A.
5797
295318582018
KCRGDCFC
[68Ga]Ga-DOTA-RGD8CH2CO chemical group attached, DOTA conjugated with Lys1CCPEGCyclic (C2-C6 Disulfide Bond)L68Ga labellingSyntheticPET imaging agent to visualize and quantify angiogenesisBlood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection1 mg/kg1.9 (Fast Phase)NHP plasma proteaseUV-HPLC and LC-ESI-MSNHP uterus plasma after administration of NC-100717 (1 mg/kg)In VivoNoneNoneN.A.
5798
295286342018
HGDGSFSDEMNTILDNLAARDFINWLIQTKITD
GLP2-2G33FreeFreeLinearLAla2 was substituted with GlyGLP-2 analogueTreatment of Short Bowel SyndromePlasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h)10 nmol/kg25Mice plasma proteaseIn vitro cell based activity assayMice plasmaIn VivoNoneNoneEC50(nM) = 0.035 ± 0.003
5803
295179112018
CSFPY-hArg-CAHQDLC
2d13AcetylationFreeBicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene)LTrp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions2a analogueAntidiabetes (Treatment of Diabetic Macular Edema)Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose,5 mg/kg48Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneKi Values (nM) = 30 ± 9 against PKal from Rats
5822
294618332018
X-RPR-X-SHKGP-Nle-PF
Pyr analogue 213FreeFreeCyclic (X1-X5 Bond)LX= allylglycine, Nle = Nor-leucinePyr-13 analogueEffects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic ShockAt selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).1 mM0.8 ± 0.2Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneKi binding (nM) = 5.7 ±3.5 for 2
5824
294618332018
X-PRL-X-HKGP-Nle-PF
Pyr analogue 413pGlu = PyroglutamateFreeCyclic (X1-X6 Bond)LX= allylglycine, Nle = Nor-leucinePyr-13 analogueEffects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic ShockAt selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min).1 mM0.7 ± 0.1Rats plasma proteaseUPLC-MSRats plasmaIn VitroNoneNoneKi binding (nM) = 523 ±165 for 4L
5836
294368352018
(hpcdypewqwlcelGk)3
PIE 12-trimer48Maleimide joined by linker PEG24FreeLinearMixAll D-amino acids except GlySyntheticAntiviral (HIV Entry Inhibitor)5 min to 24 h1 mg/kg0.6Rats plasma proteaseLC-MS/MS using an Agilent HPLCRats plasmaIn VivoNoneNoneJRFL(nM) = 2.1 ± 0.28 (antiviral potency)
5837
294368352018
(hpcdypewqwlcelGk)3
PIE 12-trimer48Maleimide joined by linker PEG24FreeLinearMixAll D-amino acids except GlySyntheticAntiviral (HIV Entry Inhibitor)15 min to 48 h1 mg/kg0.8Rats plasma proteaseLC-MS/MS using an Agilent HPLCRats plasmaIn VivoNoneNoneJRFL(nM) = 2.1 ± 0.28 (antiviral potency)
5840
294368352018
(hpcdypewqwlcelGk)3
C16-PIE12-trimer48C16-Maleimide joined by linker PEG24FreeLinearMixAll D-amino acids except GlySyntheticAntiviral (HIV Entry Inhibitor)5 min to 24 h1 mg/kg0.9Rats plasma proteaseLC-MS/MS using an Agilent HPLCRats plasmaIn VivoNoneNoneJRFL(nM) = 0.11 ± 0.012 (antiviral potency)
5866
294215642018
RPKPQQFFGLM
SP11FreeFreeLinearLNoneSyntheticTherapeutic Angiogenesis in Diabetic Hindlimb Ischemia0 to 72 h at 37°C5 nmol2Human serum proteaseELISAHuman serumIn VitroNoneNoneN.A.
5868
294215642018
RPKPQQFFGLM
SP11FreeFreeLinearLNoneSyntheticTherapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites0 to 72 h at 37°C5 nmol1.7Diabetic rats serum proteaseELISADiabetic rats serumIn VitroNoneNoneN.A.
5877
293290722018
YFLFRPRN
Compound 18FreeAmidationLinearLNoneNMU-analogsRegulation of Feeding Behavior, the stress response and nociception37 °C112 µM4.3 ± 0.2Human plasma proteaseRP-HPLCHuman plasma In VitroNoneNoneEC50(nM) = 38.9, IC50(nM) = 0.78 for hNMUR1 and EC50(nM) = 30.8, IC50(nM) = 1.7 for hNMUR2 
5885
292823032018
SIINFEKL
SCRAP-mCherryN.A.DDmCherryN.A.LNoneSyntheticAffects Antigen PresentationN.A.N.A.41 ± 5 El4 cells proteaseBD cytoflex flow cytometryEL4 cells after Shield-1 removalN.A.NoneNoneN.A.
5890
291224412018
YGGEAAREACARCEAARE
FAMP1 18FAMAmidationCyclic (C10-C13 Disulfide Bond)LNoneSyntheticN.A.37 C10 µM7293T cells lysates proteaseRP-HPLC-FD293T cells lysateIn VitroNoneNoneN.A.
5891
291224412018
YGGEAAREACARCEAARE
FAMP1 18FAMAmidationCyclic (C10-C13 Disulfide Bond)LNoneSyntheticIncreases Half Life37 C10 µM21293T cells lysates proteaseRP-HPLC-FD293T cells lysateIn VitroNoneNoneN.A.
5892
291224412018
YGGEAAREACARECAARE
FAM-P2 18FAMAmidationCyclic (C10-C14 Disulfide Bond)LNoneSyntheticN.A.37 C10 µM16293T cells lysates proteaseRP-HPLC-FD293T cells lysateIn VitroNoneNoneN.A.
5893
291224412018
YGGEAAREACARECAARE
FAM-P2.L518FAMAmidationCyclic (C10-C14 Disulfide Bond)L1,3-bis(bromomethyl)benzene linker (L5) for stapling i, i+4 spacingSyntheticIncreases Half Life37 C10 µM10293T cells lysates proteaseRP-HPLC-FD293T cells lysateIn VitroNoneNoneN.A.
5895
291041452018
ATWLPPR
AS167FreeFreeLinearLNoneSyntheticAntitumorBlood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit45 mg/kg1Rats serum proteaseELISARats serumIn VivoNoneNoneThe activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model
5896
290513422018
TGRAKRRMQYNRR
68Ga-NOTA-UBI 1368Ga-NOTAFreeLinearLNoneSyntheticNuclear Imaging of Infectious DiseasesImage acquisition started 30, 60 and 120 min after IVN.A.29NHP blood proteasePET-CT imagingNHP blood sampleIn VivoNoneNoneN.A.
5898
289482962018
EGTFISDYSIAMDKHIQDFVNWLLAQK
GIP(3-30)NH227FreeAmidationLinearLNoneGIP analogueGIP receptor antagonistBlood samples were drawn 30, 15 and 0 min before and 20, 25, 30, 40, 50, 60, 67, 70, 75, 80, 95 and 125 min after the start of the GIP(3-30)NH2 infusion800 pmol/kg/min7.6 ± 1.4 (Elimination Half Life)Human plasma proteaseRIAHuman plasmaIn VivoNoneNoneIC50 value of 87.6 nmol/l
5901
N.A.2018
(GIVEQCCHSICSLYQLENYCN-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 749FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond, B3E, desB27, modifications Insulin DerivativeTreatment of HypoglycaemiaBlood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes1 nmol/kg44Pig plasma proteaseELISAPig plasmaIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 10.5
5902
N.A.2018
(GIVEQCCTSICSLYQLENYCA-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 849FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,A21A, B3E, desB27 modificationsInsulin DerivativeTreatment of HypoglycaemiaBlood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes1 nmol/kg45Pig plasma proteaseELISAPig plasmaIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 11.8
5903
N.A.2018
(GIVEQCCTSICSLYQLENYCA-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 849FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,A21A, B3E, desB27 modificationsInsulin DerivativeTreatment of HypoglycaemiaBlood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes1 nmol/kg52Pig plasma proteaseELISAPig plasmaIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 11.8
5906
N.A.2018
(GIVEQCCTSICSLYQLENYCA-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 849FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,A21A, B3E, desB27,modificationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg29SD rats plasma proteaseELISASD rats plasma with zinc ionIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 11.8
5907
N.A.2018
(GIVEQCCHSICSLYQLENYCA-OH)-(FVEQHLCGSHLVEALYLVCGERGFFYPK)
Example 549FreeB29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,A21A, B3E, desB27, modifcationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg35SD rats plasma proteaseELISASD rats plasma with zinc ionIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 7.6
5908
N.A.2018
(GIVEQCCTSICSLYQLENYCA-OH)-(FVQQHLCGSHLVEALYLVCGERGFFYPK)
Example 949FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond, A21A, B3Q, desB27, modificationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg30SD rats plasma proteaseELISASD rats plasma with zinc ionIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 16.7
5909
N.A.2018
(GIVEQCCHSICSLYQLENYCN-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 749FreeB29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications Cyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond, B3E, desB27, modififcationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg30SD rats plasma proteaseELISASD rats plasma with zinc ionIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 10.5
5910
N.A.2018
(GIVEQCCTSICSLYQLENYCN-OH)-(FVEQHLCGDHLVEALYLVCGERGFFYPK)
Example 449FreeB29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,B3E, desB27,modificaitonsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg31SD rats plasma proteaseELISASD rats plasma with zinc ionIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 9.3
5911
N.A.2018
(GIVEQCCTSICSLYQLENYCN-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTDK)
Prior Art analogue 250FreeB29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,B28D, modifcationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg45SD rats plasma proteaseELISASD rats plasma with 3 Zinc Ion Per HexamerIn VivoNoneUS 201615754342 AN.A.
5912
N.A.2018
(GIVEQCCTSICSLYQLENYCN-OH)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK)
Prior Art analogue 350FreeB29K(N(Eps)Tetradecanedioyl), desB30 modificationsCyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond, modificationsInsulin DerivativeTreatment of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg50SD rats plasma proteaseELISASD rats plasma with 3 Zinc Ion Per HexamerIn VivoNoneUS 201615754342 AN.A.
5914
N.A.2018
(GIVEQCCTSICSLYQLENYCA-OH)-(FVQQHLCGSHLVEALYLVCGERGFFYPK)
Example 2349FreeB29K(N(Eps)Hexadecanedioyl-4×gGlu), desB30 modificationscyclic (C7-C12 disulfide bond in A chain)LA and B chain linked with disulfide bond,A21A, B3Q, desB27, modificationsInsulin DerivativeTreatment Of HypoglycaemiaPlasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing25 nmol/kg55SD rats plasma proteaseELISASD rats plasma with Zinc IonIn VivoNoneUS 201615754342 ALipogenesis 1% HSA (%rel to HI) = 1.54
5940
288998382017
GLSKGCFGLKLDRIGSMSGLGC
CNP(1-22)22FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneProduced from recombinant DNA in Escherichia coliTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.0.02 mg/kg1.96 ± 0.05Rats plasma proteaseRIARats plasma without NEP inhibitorIn VivoNoneNoneCNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22)
5941
288998382017
GLSKGCFGLKLDRIGSMSGLGC
CNP(1-22)22FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneProduced from recombinant DNA in Escherichia coliTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.0.02 mg/kg9.94 ± 1.40Rats plasma proteaseRIARats plasma with NEP inhibitorIn VivoNoneNoneCNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22)
5942
288998382017
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
CNP(6-22)ghrelin(12-28) 34FreeGhrelin (12-28)Cyclic (C1-C17 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.0.02 mg/kg14.9 ± 3.1Rats plasma proteaseRIARats plasma without NEP inhibitorIn VivoNoneNoneCNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22)
5943
288998382017
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
CNP(6-22)ghrelin(12-28) 34FreeGhrelin (12-28)Cyclic (C1-C17 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.0.02 mg/kg12.7 ± 1.2Rats plasma proteaseRIARats plasma with NEP inhibitorIn VivoNoneNoneCNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22)
5944
288998382017
GLSKGCFGLKLDRIGSMSGLGC
CNP(1-22)22FreeFreeCyclic (C6-C22 Disulfide Bond)LNoneProduced from recombinant DNA in Escherichia coliTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.10 nmol/kg4.34 ± 0.20Rats plasma proteaseRIARats plasmaIn VivoNoneNoneCNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22)
5945
288998382017
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
CNP(6-22)ghrelin(12-28) 34FreeGhrelin (12-28)Cyclic (C1-C17 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.11 nmol/kg15.03 ± 4.31Rats plasma proteaseRIARats plasmaIn VivoNoneNoneCNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22)
5946
288998382017
VQQRKESKKPPAKLQPRCFGLKLDRIGSMSGLGC
Ghrelin(12-28)CNP(6-22)34Ghrelin (12-28)FreeCyclic (C18-C34 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.12 nmol/kg17.75 ± 3.99Rats plasma proteaseRIARats plasmaIn VivoNoneNoneThe activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28)
5947
288998382017
VQQRKESKKPPAKLQPRCFGLKLDRIGSMSGLGC
Ghrelin(12-28)CNP(6-22)34Ghrelin (12-28)FreeCyclic (C18-C34 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.13 nmol/kg14.86 ± 2.64Rats plasma proteaseRIARats plasmaIn VivoNoneNoneThe activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28)
5948
288998382017
CFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
CNP(6-22)ghrelin(12-28)amide34FreeGhrelin(12-28)amideCyclic (C1-C17 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.14 nmol/kg14.50 ± 0.85Rats plasma proteaseRIARats plasmaIn VivoNoneNoneThe CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22)
5949
288998382017
VQQRKESKKPPAKLQPRCFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Ghrelin(12-28)CNP(6-22)ghrelin(12-28)51FreeGhrelin(12-28)Cyclic (C18-C34 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.15 nmol/kg18.40 ± 2.05Rats plasma proteaseRIARats plasmaIn VivoNoneNoneAgonist activity of ghrelin(12-28)CNP(6-22)ghrelin(12-28) was also the lowest
5950
288998382017
RPQLKAPPKKSEKRQQVCFGLKLDRIGSMSGLGCVQQRKESKKPPAKLQPR
Ghrelin(28-12)CNP(6-22)ghrelin(12-28) 51Reversed sequence ghrelin(28-12) fused to the N-terminal side of CNP(6-22)FreeCyclic (C18-C34 Disulfide Bond)LNoneNatriuretic peptide derivativesTreatment of Growth Failure and Short Stature Disorders such as AchondroplasiaN.A.16 nmol/kg17.38 ± 1.00Rats plasma proteaseRIARats plasmaIn VivoNoneNoneGhrelin(28-12)CNP(6-22)ghrelin(12-28) exhibited lower potency than that of ghrelin(28-12)CNP(6-22) and CNP(6-22)ghrelin(12-28)
5956
288002172017
DCLGAMRKCIPDNDKCCRPNLVCSRTHKWCKYVF
Peptide 2234FreeFreeLinearLAla5 substituition in GpTx-1derived from Grammostola porteri (Tarantula spider) (Lasiodora porteri)Potently inhibits the voltage-gated sodium channels Nav1.7/Scn9AAt 0.5, 1, 1.25, 1.5,2,3, and 4 hours post-dose, 3 mice were euthanized and then blood samples were collected 5 mg/kg0.605Mice plasma proteaseLC-MS/MSMice serumIn Vivohttps://sci-hub.se/10.1021/jm501765vNoneIC50=0.58-10 nM for GpTx-1
5957
287993262017
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneGLP-1AntidiabetesBlood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours5 mg/kg0.03NMR1 mice serum proteaseAlphaLISANMR1 mice serumIn VivoPDB id: 5VAINoneEC50 = 5.257*10-11
5961
287713552017
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
GLP-1 analogue 431FreeFreeLinearLK34R substituition at GLP-1, Conjugated with indomethacin via γGlu attached to the ε-amine of Lys26 of the GLP-1 analogGLP-1 analogsAntidiabetesBlood sampled at eight time-points within 24 h5 mL/kg55Lean mice plasma proteaseLuminescent Oxygen Channeling Immunoassay Lean mice plasmaIn VivoNoneNoneGLP-1R EC50 ± SEM (nM) = 0.068 ± 0.037
5972
287144752017
EYEKEYEACRWPARCVHQDLCG
tagPK12822tagFreeBicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128)LLys4 linked with Palm fatty acidSyntheticInhibit plasma kallikreinN.A.0.5 mg/kg0.9 ± 0.2 (T1/2a)Rats plasma proteaseRP-HPLC using a fluorescence detectorRats plasmaIn VivoNoneNoneAlbumin binding (Kd) (nM) = 720±90 for rat albumin
5974
287144752017
EYEKEYEACSRYEVDCRGRGSACG
tagUK1824tagFreeBicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128)LLys4 linked with Palm fatty acidSyntheticInhibit urokinaseN.A.0.5 mg/kg1.0 ± 0.1 (T1/2a)Rats plasma proteaseRP-HPLC using a fluorescence detectorRats plasmaIn VivoNoneNoneAlbumin binding (Kd) (nM) = 780±110 for rat albumin
5976
287144752017
ACSRYEVDCRGRGSACG
UK1817FreeFreeBicyclic(C2-C9,C9-C16 Disulfide Bond)LNoneSyntheticInhibit urokinaseN.A.0.3 mg/kg0.30 ± 0.02 (T1/2b)Rats plasma proteaseRP-HPLC using a fluorescence detectorRats plasmaIn VivoNoneNoneAlbumin binding (Kd) (nM) > 100,000 for rat albumin
5979
287144752017
EYEK(C14)EYE-(PEG24)3-XCFRLPCRQLRC
tag-3xPEG24-FXIIa inhibitorN.A.Tag-3xPEG24AmidationBi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor)LNoneSyntheticFXIIa InhibitorN.A.5 mg/kg1.0 ± 0.2 (T1/2a)Rabbit plasma proteaseRP-HPLC using fluorescence detectorRabbit plasmaIn VivoNoneNone(EC5x) at 4.2±0.5 mM
5981
287144752017
XCFRLPCRQLRC
FXIIa inhibitorN.A.Fluorescein (F) AmidationBi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor)LNoneSyntheticFXIIa InhibitorN.A.3.7 mg/kg0.21 ± 0.04 (T1/2b)Rabbit plasma proteaseA single quadrupole liquid chromatography mass spectrometer Rabbit plasmaIn VivoNoneNoneKi FXIIa = 4±0.9 nM in presence of albumin
5982
287117302017
MAFTEHSPLTPHRRDLCSRSIWLARKIRSDLTALTESYVKHQGLNKNINLDSADGMPVASTDQWSELTEAERLQENLQAYRTFHVLLARLLEDQQVHFTPTEGDFHQAIHTLLLQVAAFAYQIEELMILLEYKIPRNEADGMPINVGDGGLFEKKLWGLKVLQELSQWTVRSIHDLRFISSHQTGIP
rhCNTF187FreeFreeLinearLNoneSyntheticTreatment of Neurodegenerative or Metabolic diseasesAt different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) 1 mg/kg34.28SD rats serum proteaseELISASD rats serumIn VivoPDB id: 1CNTNoneEC50±SD = 0.48±0.12ng/ml for rhCNTF 
5997
286051802017
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicBlood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing80 µg/mL18Rats serum proteaseLC-MS/MSRats serumIn VivoPDB id: 7MLLNoneIC50(nM) = 0.21 ±0.0 for exenatide
5998
286051802017
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicBlood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing80 µg/mL50Rats serum proteaseLC-MS/MSRats serumIn VivoPDB id: 7MLLNoneIC50(nM) = 0.21 ±0.0
5999
286051802017
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide 39FreeAmidationLinearLSubstituiting Asn28 with Gln28Exenatide analogsAntidiabetesBlood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing49 µg/mL17Rats serum proteaseLC-MS/MSRats serumIn VivoPDB id: 7MLLNoneIC50(nM) = 11 ±3.7
6000
286051802017
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
[Gln28]exenatide 39FreeAmidationLinearLSubstituiting Asn28 with Gln28Exenatide analogsAntidiabetesBlood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing49 µg/mL48Rats serum proteaseLC-MS/MSRats serumIn VivoPDB id: 7MLLNoneIC50(nM) = 11 ±3.7
6016
284640432017
YNWNSFGLRF
KP-1010FreeAmidationLinearLNonekisspeptin analogueTreatment of Specific Human Reproductive Disorders100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min)1 nmol4Mouse plasma proteaseRIAMouse plasmaIn Vivohttps://www.jbc.org/article/S0021-9258(19)77047-1/fulltextNoneN.A.
6017
284640432017
GTSLSPPPESSGSPQQPGLSAPHSRQIPAPQGAVLVQREKDLPNYNWNSFGLRF
KP-5454FreeAmidationLinearLNonekisspeptin analogueTreatment of Specific Human Reproductive Disorders100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min)1 nmol32Mouse plasma proteaseRIAMouse plasmaIn Vivohttps://www.jbc.org/article/S0021-9258(19)77047-1/fulltextNoneN.A.
6018
284578952017
HGEGTFTSDLSKQMEEEAVRLFIEWLKQGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemic1 hour25 nmol/kg~0.35ICR mice retro-orbital sinus proteaseExenatide ELISAICR mice retro-orbital sinusIn VivoPDB id: 7MLLNoneboth exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity
6022
284167442017
RGDyK
cRGD-ZW800-15FreeZW800-1 fluorophoreCyclic (RGDyK)Mixy = D-TyrSyntheticGeneric tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid TumorsTime points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection10 nmol25.3 ± 6.4Mice serum proteaseFluorescence assayMice serumIn VivoNoneNoneIn vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD 
6025
283739722017
ONNRPVYIPRPRPPHPRL
Api8818Gu: N,N,N',N' tetramethylguanidinoAmidationLinearLO denotes L-ornithineApidaecin analogAntibacterialAfter 10, 20, 30, 60, or90 min animals (n = 7)5 mg/kg17.3Mice plasma proteaseRP-HPLC-ESI-MSMice plasmaIn VivoNoneNoneMIC = Api88 > Api137
6026
283739722017
ONNRPVYIPRPRPPHPRL
Api8818Gu: N,N,N',N' tetramethylguanidinoAmidationLinearLO denotes L-ornithineApidaecin analogAntibacterialAfter 10, 20, 30, 60, or90 min animals (n = 7)20 mg/kg11.1Mice plasma proteaseRP-HPLC-ESI-MSMice plasmaIn VivoNoneNoneMIC = Api88 > Api137
6027
283739722017
ONNRPVYIPRPRPPHPRL
Api13718Gu: N,N,N',N' tetramethylguanidinoFreeLinearLO denotes L-ornithineApidaecin analogAntimicrobialAfter 10, 20, 30, 60, or90 min animals (n = 7)5 mg/kg33.8Mice plasma proteaseRP-HPLC-ESI-MSMice plasmaIn VivoNoneNoneThe minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL.
6028
283739722017
ONNRPVYIPRPRPPHPRL
Api13718Gu: N,N,N',N' tetramethylguanidinoFreeLinearLO denotes L-ornithineApidaecin analogAntimicrobialAfter 10, 20, 30, 60, or90 min animals (n = 7)20 mg/kg16.9Mice plasma proteaseRP-HPLC-ESI-MSMice plasmaIn VivoNoneNoneThe minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL.
6036
282818682017
MALCKFCDVRFSTCDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPTCIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPD
eTGFBR2112FreeFreeLinearLNoneSyntheticNeutralize TGF-Β1 activityBlood samples were collected through the eyes at 5 min, 15 min, 30 min, 60 min, 120 min3 nmol/kg41.42Mice serum proteaseHuman TGF-b RII Duo Set ELISA Mice serumIn VivoNoneNoneKD = 9.49* 10-9M of eTGFBR2 for TGF-B1
6038
282094192017
HADGSFSDEMNTILDNLAARDFINWLIQTKITD
Native GLP-233FreeFreeLinearLNoneGlucagonTreatment of Short Bowel Syndrome Samples were taken prior to GLP-2 administration and at 60, 90 and 180 min post injection on Day 3 of therapy or Day 422.5 μg/kg~45Human plasma proteaseGLP-2 (1–33) specific radioimmunoassayInfant human plasmaIn VivoPDB id: 2L63NoneN.A.
6039
281387432017
ILKKWPWWPWRRK
CP-1113FreeAmidationLinearLNoneSyntheticAntimicrobialA plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h)10 μM0.21Mouse plasma proteaseLC-HRMS.Mouse plasmaIn VitroNoneNoneN.A.
6040
281387432017
ILRWPWWPWRRK
Omiganan13FreeAmidationLinearLNoneAnalogue of indolicidinAntimicrobialA plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h)10 μM0.83Mouse plasma proteaseLC-HRMS.Mouse plasmaIn VitroNoneNoneN.A.
6042
280976292017
AGYKPDEGKRGDACEGSDGGPFV
TP50823FreeAmidationLinearLTAMRA-labeledSyntheticTreatment of Diabetic Foot UlcersN.A.2.16 mM13.7Male CD1 mice plasma proteaseFluorescence assayMale CD1 mice plasmaIn VivoNoneNoneN.A.
6043
280976292017
AGYKPDEGKRGDACEGSDGGPFV
PEG5k-TP50823PEG5KAmidationLinearLTAMRA-labeledSyntheticTreatment of Diabetic Foot UlcersN.A.2.16 mM11.5Male CD1 mice plasma proteaseFluorescence assayMale CD1 mice plasmaIn VivoNoneNoneN.A.
6052
280108442017
fCFwKTCT
Octreotide8D-amino acid PheFreeCyclic (C2-C7 Disulfide Linkage)MixD-amino acid substituitons TrpSST analogAnticancer and treatment of Endocrine Diseases The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min50 mg/kg28Mouse stomach tissue lysate proteaseHPLC-MSMouse stomach tissue lysateIn Vivohttps://sci-hub.st/10.1177/106002808802201001NoneN.A.
6053
280108442017
fCFwKTCT
Octreotide8D-amino acid PheFreeCyclic (C2-C7 Disulfide Linkage)MixD-amino acid substituitons TrpSST analogAnticancer and treatment of Endocrine Diseases The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min50 mg/kg37.7Mouse intestine tissue lysate proteaseMALDI-TOF-MSI and LC-MS/MSMouse intestine tissue lysateIn VivoNoneNoneN.A.
6066
278153372017
pGlu-RPRLSHKGPMPF
pE13F13pGlu = PyroglutamateFreeLinearLNoneApelin analogsDiuretic and Cardiovascular Effects37°C5 μM 7.2Mouse plasma proteaseLC-MSMouse plasmaIn VitroNoneNoneRecruitment of b-arrestin2 by BRET, EC50 (nM) = 300 ± 182
6068
278153372017
KFRRQRPRLSHKGPMPF
K17F17FreeFreeLinearLNoneApelin analogsDiuretic and Cardiovascular Effects37°C5 μM 4.6Mouse plasma proteaseLC-MSMouse plasmaIn VitroNoneNoneRecruitment of b-arrestin2 by BRET, EC50 (nM) = 15 ± 3.6
6069
278153372017
KFaRqRPRlS-Aib-Ka-ProNle-PF
P9217AcetylationPro(4-Br)Phe substituitionLinearMixAib, DLeu,DGln, ProNle, D-Arg at position 3Apelin analogsDiuretic and Cardiovascular Effects37°C5 μM 24Mouse plasma proteaseLC-MSMouse plasmaIn VitroNoneNoneRecruitment of b-arrestin2 by BRET, EC50 (nM) = 4 ± 2.4
6071
277846922017
MCGPGVG-(VPGxG)160-VPGWPGSG
ELP815FreeFreeLinearLx = Val,Gly or AlaSyntheticCarrier proteinWhole-animal fluorescence images were collected at regular intervals for 24 hours100 mg/kg52.6 (T1/2,Terminal)Rats plasma proteasewhole-body fluorescence imaging Rats plasmaIn VivoNoneNoneKTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours
6075
276894062017
HSQGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNoneProduced by the alpha cells of the pancreasAntidiabetesA total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min30 nmol/ml3.2Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoNoneNoneN.A.
6076
276894062017
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
GLP-131FreeFreeLinearLNoneSyntheticAntidiabetesA total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min30 nmol/ml1.2Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoPDB id: 5VAINoneN.A.
6077
276894062017
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exendin-439FreeAmidationLinearLNoneExendin-4AntidiabetesA total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min30 nmol/ml35.1Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoPDB id: 7MLLNoneEC50 (pM) = 1.8 ± 0.8
6078
276894062017
N.A.
X1N.A.N.A.N.A.N.A.N.A.N.A.N.A.AntiobesityN.A.N.A.3.9Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoNoneNoneN.A.
6079
276894062017
N.A.
X2N.A.N.A.N.A.N.A.N.A.N.A.N.A.AntiobesityN.A.N.A.16.1Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoNoneNoneN.A.
6080
276894062017
N.A.
X3N.A.N.A.N.A.N.A.N.A.N.A.N.A.AntiobesityN.A.N.A.21.3Surgical rats plasma protease (Wistar Rat)RIASurgical rats plasma (Wistar rat)In VivoNoneNoneN.A.
6081
275391572017
VEPNCDIHVMWEWECFERL-Tz4-lfreW
Anti‐VEGF PCCs Bi‐LV23X1 = biotin-PEG3 labellfreW = D and L -amino acidsCyclicMixTz4 = triazole linkerSyntheticIn vivo imaging probe and an Anti‐PA peptideBlood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min1 mg/kg7 (Elimination Half Life)Mice plasma proteaseLC‐MS/MS assayMice plasmaIn VivoNoneNoneN.A.
6082
275391572017
VEPNCDIHVMWEWECFERL-Tz4-eeird
Anti‐VEGF PCCs Tri‐LV28X1 = biotin-PEG3 labeleeird = D-amino acidsCyclicMixTz4 = triazole linkerSyntheticIn vivo imaging probe and an Anti‐PA peptideBlood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min1 mg/kg36 (Elimination Half Life)Mice plasma proteaseLC‐MS/MS assayMice plasmaIn VivoNoneNoneIC50 = 2.6 ± 0.5 nM
6083
N.A.2017
ASDEEIQDVSGTWYLKAMTVDRFKIASWPRSVTPMTLTTLEGGNLEAKVTMNWWGRSQEVKAVLERTDEPGKYTAQGDRHVAYIIRSPVKDHYIFYSEGNLQGETVPGVWLVGRDPKNNLEALEDFEKAAGARGLSTESILIPRQSETSSPG
SEQ ID NO 62152FreeFreeLinearLNoneLipocalin muteins Pcsk9-Specific Lipocalin MuteinsN.A.N.A.0.99Rats plasma proteaseSandwich ELISARats plasmaIn VivoNoneUS 201715445066 AIC50(nM) = 1.36 without HSA for LDLR binding
6084
N.A.2017
GASDEEIQDVSGTWYLKAMTVDRFKIASWPRSVTPMTLTTLEGGNLEAKVTMNWWGRSQEVKAVLERTDEPGKYTAQGDRHVAYIIRSHVKDHYIFYSEGNLQGETVPGVWLVGRDPKNNLEALEDFEKAAGARGLSTESILIPRQSETSSPG
SEQ ID NO 82153FreeFreeLinearLNoneLipocalin muteins Pcsk9-Specific Lipocalin MuteinsN.A.N.A.0.86Rats plasma proteaseSandwich ELISARats plasmaIn VivoNoneUS 201715445066 AIC50(nM) = 1.68 without HSA for LDLR binding
6112
275582962016
pGlu-RPRLSHKGPMPF
Compound 113pGlu = PyroglutamateFreeLinearLNoneApelin analogsInotropic AgentTime points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h)1 µg/mL 0.025Wistar rats plasma proteaseESI-MSWistar rats plasmaIn VitroNoneNoneEC50(nM) = 2.6 ± 1.0 
6113
275582962016
pGlu-RPRLSHKGP-Nle-PF
Compound 213pGlu = PyroglutamateFreeLinearLNle = Norleucine at position 11Apelin analogsInotropic AgentTime points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h)1 µg/mL 0.13Wistar rats plasma proteaseESI-MSWistar rats plasmaIn VitroNoneNoneEC50(nM) = 2.0 ± 0.3 
6114
275582962016
pGlu-CRPRLCHKGP-Nle-PF
Compound 2614pGlu = PyroglutamateFreeCyclic (C2-C7 Disulfide Linkage)LNle = Norleucine at position 12Apelin analogsInotropic AgentTime points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h)1 µg/mL 0.1Wistar rats plasma proteaseESI-MSWistar rats plasmaIn VitroNoneNoneEC50(nM) > 1000
6117
275582962016
QRPRLSHKKP-Nle-Aib-F
Compound 3113Palmitic acid conjugationFreeLinearLGly9 was exchanged with Lys, TAMRA = 5,6-carboxytetramethylrhodamine at Lys9 modification at Lysine , Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12compound 31 analoguesInotropic Agent37 C0.00001 M0.36Wistar rats plasma proteaseHPLCWistar rats plasmaIn VitroNoneNoneEC50(nM) = 21.6 ± 4.5 for compound 31
6129
272175902016
CYIQNCPLG
OT (oxytocin)9FreeAmidationCyclic (C1-C6 Disulfide Linkage)LNoneProduced in the hypothalamus and released by the posterior pituitary glandTreatment of Psychiatric Diseases, Including Autism Spectrum Disorders And SchizophreniaTime points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours0.1 mg/kg0.12Wistar rats plasma proteaseLC-MS/MS Wistar rats plasmaIn Vivohttps://sci-hub.st/10.1016/s0079-6123(08)00417-2NoneEC50(nM) = 0.039 (OTR agonist)
6132
272175902016
CYIQNCPLG
OT (oxytocin)9FreeAmidationCyclic (C1-C6 Disulfide Linkage)LNoneProduced in the hypothalamus and released by the posterior pituitary glandTreatment of Psychiatric Diseases, Including Autism Spectrum Disorders And SchizophreniaTime points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only10 ml/kg0.5C57Bl/6J mice plasma proteaseLC-MS/MS C57BL/6J mice plasma In VivoPDB id: 2MGONoneEC50(nM) = 0.039 (OTR agonist)
6138
271669822016
GGCRFGTCTVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
ADM analogue 3 39Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 AmidationCyclic (C3-C8 Disulfide Linkage)LNoneADM analogueTreatment of Cardiovascular Diseases37°C0.00001 M3.3Porcine liver homogenate proteaseRP-HPLCPorcine liver homogenate In VitroNoneNoneEC50 = 13.2 nM for ADM analogue 15
6139
271669822016
KG-Dpr-RFGTETVQKLAHQIYQFTDKDKDNVAPRSKISPQGY
ADM analogue 2038Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 AmidationCyclic (Dpr3-E8 Lactam Bridge)LNα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 ADM analogueTreatment of Cardiovascular Diseases37°C0.00001 M38Porcine liver homogenate proteaseRP-HPLCPorcine liver homogenate In VitroNoneNoneEC50 = 13.2 nM for ADM analogue 15
6160
268180562016
YPAKPEAPGEDASPEELSRYYASLRHYLNLVTRQRY
PYY1–3636FreeAmidationLinearLNoneReleased from enteroendocrine cellsAnorexic effectsBlood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 minPYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–3610.1 ± 0.5 (Elimination Half Life)Human blood plasma proteaseRIAHuman blood plasma with 2 × 100 mg sitagliptinIn Vivohttps://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.xNoneThe human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l
6161
268180562016
YPAKPEAPGEDASPEELSRYYASLRHYLNLVTRQRY
PYY1–3636FreeAmidationLinearLNoneReleased from enteroendocrine cellsAnorexic effectsBlood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 minPYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–369.4 ± 0.8 (Elimination Half Life)Human blood plasma proteaseRIAHuman blood plasmaIn Vivohttps://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.xNoneThe human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l
6162
268180562016
AKPEAPGEDASPEELSRYYASLRHYLNLVTRQRY
PYY3-3634FreeAmidationLinearLNoneReleased from enteroendocrine cellsAnorexic effectsBlood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 minPYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–3614.9 ± 1.3 (Elimination Half Life)Human blood plasma proteaseRIA (total PYY assay)Human blood plasmaIn Vivohttps://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.xNoneThe human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l
6166
268081992016
LRHWLNLLTRQRW
PYY24–3613FreeAmidationLinearLNonePYY analogAntiobesityAn amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point1000 ng/mL<0.5SD rats plasma proteaseLC–MS/MSSD rats plasmaIn VitroNoneNoneHSA binding correlated well with plasma stability
6178
267745882016
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQR
PYY3-3533FreeFreeLinearLNoneIsolated and purified from porcine small intestineDecrease appetite and food-intakeConducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min1 µM6Minipigs heparin-plasma proteaseLC-MSminipigs heparin-plasma In VitroNoneNoneN.A.
6179
267745882016
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQR
PYY3-3533FreeFreeLinearLNoneIsolated and purified from porcine small intestineDecrease appetite and food-intakeConducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min1 µM39Minipigs heparin-plasma proteaseLC-MSminipigs heparin-plasma with 10 mM EDTAIn VitroNoneNoneN.A.
6182
267520862016
GGLRSLGRKILRAWKKYGQRLGNQWAVGHLM
BB2831conjugating a truncated antimicrobial peptide B28 to the N-terminus of the tumor-homing peptide bombesinAmidationLinearLBiotinylationSyntheticAntitumorN.A.30 nmol<5BALB/c mice plasma proteaseELISABALB/c mice plasmaIn VivoNoneNoneIC50 ranges from 2.5–3.0 mM (In the absence of FBS) for BB28
6183
267414582016
FEFQFK
Peptide 1 6FreeFreeLinearLNoneSyntheticHydrogelatorsDegradation was monitored after 0, 1, 2, 3, 4, 5, and 10 min34 μM3.43 ± 0.06Human blood plasma proteaseHPLCHuman blood plasmaIn VitroNoneNoneN.A.
6184
267414582016
FE-β3hF-FQ-β3hF-FK
Peptide 28FreeFreeLinearLβ3-homophenylalanine (β3-hPhe) at position 3 and 6SyntheticHydrogelatorsDuring the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.33 μM19.53 ± 0.55Human blood plasma proteaseHPLCHuman blood plasmaIn VitroNoneNoneN.A.
6185
267414582016
FE-β3hF-FQ-β3hF-FK
Peptide 38FreeAmidationLinearLβ3-homophenylalanine (β3-hPhe) at position 3 and 6SyntheticHydrogelatorsDuring the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.33 μM40.00 ± 1.28Human blood plasma proteaseHPLCHuman blood plasmaIn VitroNoneNoneN.A.
6186
267414582016
FE-β3hF-YQ-β3hF-YK
Peptide 48FreeAmidationLinearLβ3-homophenylalanine (β3-hPhe) at position 3 and 6, substitution of Phe with Tyr at positions 4 and 7SyntheticHydrogelatorsDuring the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min.33 μM18.71 ± 0.44Human blood plasma proteaseHPLCHuman blood plasmaIn VitroNoneNoneN.A.
6187
267254262016
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicN.A.23.88 nmol/mL0.05784ChymotrypsinMass spectrometryIntestinal fluid buffer (pH 6.8) with Chymotrypsin (0.2 U/mL)In VitroPDB id: 7MLLNoneN.A.
6223
266285552016
TGENHR
HLDF-6-NH263H labeling at N terminalAmidationLinearLNoneIsolated from the culture medium of retinoic acid-treated HL-60 cellsNeuroprotective And Nootropic ActivitiesN.A.N.A.8Wistar rats blood plasma proteaseN.A.Wistar rats blood plasmaIn VivoNoneNoneChAT activity, dpm/mg of tissue = 5.61±0.40 in (βA + HLDF-6-NH2,250 µg/kg)
6224
266285552016
TGENHR
HLDF-6-OH 63H labeling at N terminalFreeLinearLNoneIsolated from the culture medium of retinoic acid-treated HL-60 cellsNeuroprotective And Nootropic ActivitiesN.A.N.A.2Wistar rats blood plasma proteaseN.A.Wistar rats blood plasmaIn VivoNoneNoneChAT activity, dpm/mg of tissue = 5.29±0.34 in (βA + HLDF-6-OH,250 µg/kg)
6239
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose20 mg5.9Human serum proteaseHPLC–MS/MSHuman serum (Japanese)In VivoPubchem id: 86278343NoneN.A.
6240
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose80 mg13.7Human serum proteaseHPLC–MS/MSHuman serum (Japanese)In VivoPubchem id: 86278343NoneN.A.
6241
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose240 mg23.5Human serum proteaseHPLC–MS/MSHuman serum (Japanese)In VivoPubchem id: 86278343NoneN.A.
6242
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose20 mg6.9Human serum proteaseHPLC–MS/MSHuman serum ( Caucasians)In VivoPubchem id: 86278343NoneN.A.
6243
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose80 mg14.4Human serum proteaseHPLC–MS/MSHuman serum ( Caucasians)In VivoPubchem id: 86278343NoneN.A.
6244
262423822016
ARRCYNDPKCSDFVQADE
JNJ-5445284018FreeFreeCyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage)LNoneSyntheticTreatment for Chronic Heart FailureBlood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose240 mg26.1Human serum proteaseHPLC–MS/MSHuman serum ( Caucasians)In VivoPubchem id: 86278343NoneN.A.
6258
133-353-120-049-1212016
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALRAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDRVEPKSGDKTSTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGPFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPGK
rHuEPO-Fc399FreeFreeLinearLFusion with IgG Fc fragmentHuman erythropoietic protein Fusion with IgG Fc fragmentImmunogenicN.A.5 ug/kg 35.24+/-5.15Not mentionedELISABloodin vivohttps://lens.org/133-353-120-049-121US 9,375,487 B2N.A.