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Browsing by half-Life: Between 36001 to 54000 Seconds

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IDPMIDYEARSequenceNameLengthN-ter MODC-ter MODLinear/CyclicChiralityChem-MODOriginNatureIncubation TimeConcentrationHalf LifeUnits Half LifeProteaseAssayTest SampleVivo/VitroReferencePatent No.Activity
1069
150125922004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-acetyl-GLP-130AcetylationFreeLinearLNoneGlucagonAntihyperglycaemic, insulinotropicNot reported2mM peptide incubated with 1.25 mU of DPP IV>12DPP IVLC/MS equipped with a microbore C-18 HPLCDPP IVin vitroNoneNoneInsulinotropic activity in vitro at 5 ·6 mM glucose
1070
150125922004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-pyroglutamyl-GLP-130PyroGlutamic acid at 1st positionFreeLinearLNoneGlucagonAntihyperglycaemic, insulinotropicNot reported2mM peptide incubated with 1.25 mU of DPP IV>12DPP IVLC/MS equipped with a microbore C-18 HPLCDPP IVin vitroNoneNoneInsulinotropic activity in vitro at 5 ·6 mM glucose
1072
150125922004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-acetyl-GLP-130AcetylationFreeLinearLNoneGlucagonAntihyperglycaemic, insulinotropicNot reported2mM peptide incubated with 7.5 µl of human plasma>12Human plasma proteasesLC/MS equipped with a microbore C-18 HPLCHuman plasmain vitroNoneNoneInsulinotropic activity in vitro at 5 ·6 mM glucose
1073
150125922004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-pyroglutamyl-GLP-130PyroGlutamic acid at 1st positionFreeLinearLNoneGlucagonAntihyperglycaemic, insulinotropicNot reported2mM peptide incubated with 7.5 µl of human plasma>12Human plasma proteasesLC/MS equipped with a microbore C-18 HPLCHuman plasmain vitroNoneNoneInsulinotropic activity in vitro at 5 ·6 mM glucose
1082
110994872000
RQIKIWFQNRRMKWKKNELKRAFAALRDQI
Int-H1-S6A,F8A30FreeFreeLinearLNoneC-Myc derivativeAntiproliferative and proapoptoticNot reportedNot mentioned11.95Fetal calf serum proteasesHPLCFetal bovine serum batch1in vitroNoneNoneNot reported
1107
152468692004
H-Abu-EGTFTSDVSSYLEGQAAKEFIAWLVKGR
(Abu8)GLP-130FreeFreeLinearL2-aminobutyric acid (Abu)SyntheticPotentiate postprandial insulin secretion and glucose clearance12 hours2mM>12Human plasma proteaseRadioimmunoassayHuman plasmain vitroNoneNonecAMP EC50=4.7 ±1.3nM
1110
152468692004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
GLP-130FreeFreeLinearLNoneGlucagon-like peptide-1(7-36)amidePotentiate postprandial insulin secretion and glucose clearance12 hours2mM>12Human plasma proteases except DPPRadioimmunoassayHuman plasma+DPA (DPA is DPP inhibitor)in vitroNoneNonecAMP EC50=6.1 ±1.8nM
1111
152468692004
YAEGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ
GIP42FreeFreeLinearLNoneGastrointestinal incretin hormonePotentiate postprandial insulin secretion and glucose clearance12 hours2mM>12Human plasma proteases except DPPRadioimmunoassayHuman plasma+DPA (DPA is DPP inhibitor)in vitro8446620NonecAMP EC50=21.8 ±1.5nM
1178
147597712004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-acetyl-GLP-130AcetylationAmidationLinearLNoneDerivative of glucagon-like peptide-1Regulate blood glucose12 hours2 mM>12Purified DPP IVESI-MSPurified DPP IVin vitroNoneNone12 ±0.4% insulin intensity in ARIP cells
1180
147597712004
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
N-acetyl-GLP-130AcetylationAmidationLinearLNoneDerivative of glucagon-like peptide-1Regulate blood glucose12 hours2 mM>12Serum proteasesESI-MSSerumin vitroNoneNone16 ±0.1% glucokinase intensity in ARIP cells
1214
211145992010
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
hGLP-1(7-36)NH230FreeAmidationLinearLNoneGlucagon like peptide-1Regulate blood glucoseNot mentionedNot mentioned10.3Human plasma proteasesHPLCHuman plasmain vitro14759771NoneEC50=0.08 ±0.03nM for cAMP stimulation
1215
211145992010
H-Aib-EGTFTSDVSSYLEGQAAKEFIAWLVKGR
[Aib8]hGLP-1(7-36)NH230FreeAmidationLinearLAib--Aminoisobutyric acidAnalogue of glucagon like peptide-1Regulate blood glucoseNot mentionedNot mentioned12.1Human plasma proteasesHPLCHuman plasmain vitro14759771NoneEC50=0.29 ±0.22nM for cAMP stimulation
1831
176408992007
TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAILREL
T-26722538FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg12.4Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.019 µg/ml against IIIB virus
1832
176408992007
TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAILREL
T-26722538FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg12.4Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.043 µg/ml against 098 virus
1833
176408992007
TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAILREL
T-26722538FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg12.4Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.079 µg/ml against 098-T20 virus virus
1834
176408992007
TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAILREL
T-26722538FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg12.4Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.038 µg/ml against 098-T1249 virus
1835
176408992007
TTWEAWDRAIAEYAARIEALIRALQEQQEKNEAILREL
T-26722538FreeFreeLinearLNoneSynthetic peptideAntiviral peptideNot reported~1 €“2mg/kg12.4Monkey blood proteasesRP-HPLC and ESI-MSMale cynomolgus monkey blood plasma (Intravenous)in vivoNoneNoneIC50=0.196 µg/ml against 098-T651 virus
2008
155879342004
SPKMVQGSGCFGRKMDRISSSSGLGCKVLRRH
AlbuBNP32Human serum albuminFreeLinearLNoneB-type cardiac natriuretic peptides fused to HAS at N-terminalVasodilatorNot reported2.19 mg/kg11.2Mouse blood proteasesEIAMice plasma (Intravenous injection)in vivoNoneNoneEC50 =28.4 ± 1.2 nM
2051
195337222009
NPVENMMDRDSQ
C612FreeFreeLinearLNoneSynthetic peptideMimic putative inhibitor epitopes (mimotopes),Not reported150 µM~12Human plasma proteasesELISAHuman plasmain vitroNoneNoneIC50 =30 €“50 µM
2087
N.A.2004
ELAGIGILTV
[NMeEI, amide]-Melan-A10FreeAmidationLinearLMethylation of nitrogen of amide bond b/w Glu1 and Leu2 (NMe)Melan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM12Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 1 nM
2088
N.A.2004
pGlu-LAGIGILTV
[pEI, amide]-Melan-A10PyroGlutamic acid at 1st positionAmidationLinearLPyroglutamic acidMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM11Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 0.3 nM
2090
N.A.2004
ALAGIGILTV
[βAl, amide] -Melan-A10Beta-Alanine1AmidationLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM11Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 0.03 nM
2094
N.A.2004
DLAGIGILTV
[βDl, amide] -Melan-A10Beta-Asp1AmidationLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM12Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 10 nM
2096
N.A.2004
GLAGIGILTV
[NOHG1, amide]-Melan-A10Hydroxylation of N-terminal of GlycineAmidationLinearLNoneMelan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM13Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= 0.04 nM
2099
N.A.2004
ELAGIGILTV
[αMeL2, V10-amide]-Melan-A10FreeAmidationLinearLMethylation of carboxyl of Leu2Melan peptide which binds to HLAImmunogenic and HLA binding peptidesN.A.25 nM12Human serum proteasesHPLC-ESI-MSSerum (human)in vitroNoneEP1395276A1EC50= isomer1(2.5 nM); isomer2(0.1 nM)
2442
75225851994
rPKPfQwFwLLRPKPQQFFGLM
Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP22FreeFreeLinearMixNoneSubstance P (SP) analogueAnticancer drugs1, 2, 5 and 24 hours0.1 μg/ml11.8SCLC proteasesRP-HPLC and Electrochemical DetectionSmall cell lung cancer (SCLC)in vitroNoneNoneAct as growth factors
2447
75225851994
RwFWLMRPKPQQFFGLM
Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11)17FreeFreeLinearMixMethylation of phenylalanine at 3rd positionSubstance P (SP) analogueAnticancer drugs1, 2, 5 and 24 hours0.1 μg/ml14.6Mouse liver proteasesRP-HPLC and Electrochemical DetectionMouse liver homogenatein vitroNoneNoneAct as growth factors
2497
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)31FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours1.25 μg/kg14Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2498
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)32FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours2.5 μg/kg11Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2500
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)34FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours5.0 μg/kg15Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2501
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)35FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours10 μg/kg14Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2502
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)36FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours12.5 μg/kg12Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2503
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)37FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours15 μg/kg13Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2504
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)38FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours17.5 μg/kg11Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2505
121452412002
HAEGTFTSDVSSYLEGQAAKEFIAWLVRGRG
NN2211 (Glucagon- Like Peptide 1 Derivative)39FreeFreeLinearLγ-Glu-palmitoyl residue at position 21Glucagon-like peptide 1 (GLP-1) derivativeAnti-diabetic peptide48 hours20 μg/kg11Dipeptidyl peptidase IV (DPP-IV), human blood proteasesNot mentionedSubcutaneously injected in Humansin vivohttps://www.bachem.com/api-products/generic-apis/lNoneSignificant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels.
2510
198055672010
CYTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF
Enfuvirtide-PEG12-CP37AcetylationFreeLinearLMal-PEG12-CP was conjugated to Cys-enfuvirtideEnfuvirtide conjugateAntiretroviral fusion inhibitor5, 15, and 30 min and 1, 2, 4, 8, 24, and 48 h after drug injectiondose, 4 mg/kg of body weight10.4Wistar rats blood proteaseLC-MS/MSFemale Wistar ratsin vivoNoneNoneThe enfuvirtide-CP conjugates displayed similar EC50s that ranged from 51 nM to 72 nM
2522
176820732007
NQEEVSPYTLLKG
NC10066813AcetylationTc chelator (NC100194)LinearLTyr residue at 8 position is IodionatedCell penetrating peptides-Phosphorodiamidate morpholino oligomersTracer tested for nuclear medical imaging1, 1.5, 3, 6, 12, and 24 hours20, 100, 500, 1000, and 2000 μg10.5 (terminal elimination)Human plasma proteasesLC-MSInjected in human plasmain vivoNoneNoneNot reported
2571
82184821993
YRGDS
RGD containing peptide5FreeFreeLinearLI125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymerExtra Cellular Matrix proteinsAntitumor peptideNot mentioned0.2 mL11.3 (t1/2 second phase)Mice blood proteasesRadioimmunoassayIntravenously injected to C57BL6 micein vivoNoneNoneLess effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface.
2602
169823232006
(GGLYACHMGPITX1AVCQPLRX2)2Beta-ala-PEG
Hematide42AcetylationBeta-alanine-PEGLinearLX1-Napthyl-alanine, X2-SarcosineSynthetic dimeric peptideErythropoiesis stimulating agentNot mentioned0.02 mg/kg14.6 ±4.3Monkey plasma proteasesCompetitive ELISAMonkey plasma (Dose i/v adminstered)in vivoNoneNoneIC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation
2691
250393582014
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Coumarin-modified GLP-1 derivative 630FreeAmidationLinearLX-1 = Cys- conjugated-7-hydroxyCoumarin maleimideAnalog of human GLP-1Hypoglycaemic37 °C for 2-72 hours1000ng/ml15Rat plasma proteasesLC-MS/MSRat Plasmain vitroNoneNoneGLP-1 receptor Activation potency with EC50 = 18.1 ± 0.9 pM in HEK-293 cells
2693
250393582014
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Coumarin-modified GLP-1 derivative 830FreeAmidationLinearLX-1 = Cys- conjugated-7-hydroxyCoumarin maleimideAnalog of human GLP-1Hypoglycaemic37 °C for 2-72 hours1000ng/ml12.9Rat plasma proteasesLC-MS/MSRat Plasmain vitroNoneNoneGLP-1 receptor Activation potency with EC50 = 7.1 ± 0.9 pM in HEK-293 cells
2695
250393582014
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGR
Coumarin-modified GLP-1 derivative 1030FreeAmidationLinearLX-1 = Lys- conjugated-7-hydroxyCoumarin maleimideAnalog of human GLP-1Hypoglycaemic37 °C for 2-72 hours1000ng/ml11.8Rat plasma proteasesLC-MS/MSRat Plasmain vitroNoneNoneGLP-1 receptor Activation potency with EC50 =12.1 ± 0.5 pM in HEK-293 cells
2700
250393582014
HAEGTFTSDVSSYLEGQAAK(γ-Glu-palmitoyl)EFIAWLVRGRG
Liraglutide31FreeFreeLinearLγ-Glu-palmitoyl at 21 st positionAnalog of human GLP-1GLP-1 receptor agonist37 °C for 2-72 hours1000ng/ml14 .9 ±0.9Rat plasma proteasesLC-MS/MSRat Plasmain vivoNoneNoneGLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells
2710
258943762015
PlLQAtLGGGS
P32 (Fibroblast growth factor 2- binding peptide derivative)11FreeAmidationLinearMixNoneFibroblast growth factor 2- binding peptide derivativeAnti-proliferative37 °C for 1-48hours0.3478μM12Human plasma proteasesHPLCHuman plasmain vitroNoneNoneP32 significantly inhibited the proliferation of SGC-7901, MGC-803, and KATOIII cells induced with 20ng/ml of FGF2, and the IC50 values of P32 were 0.77, 1.69, and 1.09 μmol/L, respectively
2721
257710002015
MWQRPSSWIEGRFPHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY
MHDBAY (Recombinant PACAP-derived peptide)45FreeFreeLinearLNoneSynthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide)Insulin secretion stimulant0.5-24 hours0.5 mg/kg12.19db/db mice plasma proteasesLC-MS/MS(Dose i/v injected)Mice plasmain vivoNoneNoneAUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control
2722
257710002015
MWQRPSSWIEGRFPHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY
MHDBAY (Recombinant PACAP-derived peptide)45FreeFreeLinearLNoneSynthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide)Insulin secretion stimulant0.5-24 hours0.5 mg/kg>12Rabbit plasma proteasesLC-MS/MSNew Zealand White Rabbit plasma (Dose i/v injected)in vivoNoneNoneAUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control
2732
261979312015
YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
Porcine-PYY(1-36)36FreeFreeLinearLNoneSynthetic peptide hormone released from enteroendocrine cellsAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)37 °C for 24 hoursNot mentioned10.8 ±0.8Pig blood proteasesRadioimmunoassay and HPLCFemale pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotininin vitroNoneNoneHuman PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L
2734
261979312015
YPIKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
Porcine-PYY(1-36)36FreeFreeLinearLNoneSynthetic peptide hormone released from enteroendocrine cellsAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)37 °C for 24 hoursNot mentioned11.9 ±0.7Pig plasma proteasesRadioimmunoassay and HPLCFemale pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotininin vitroNoneNoneHuman PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L
2737
262221802015
HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR
G36A or [GLP-1(7-36A)]30FreeAmidationLinearLNoneGlucagon-like peptide 1 (GLP-1)Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Room Temp0.4 µM13 ±0.7Human plasma proteases + DPP IVMSHuman Plasma+ Heparinin vitroNoneNoneNot reported
2742
262221802015
HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR
G36A or [GLP-1(7-36A)]30FreeAmidationLinearLNoneGlucagon-like peptide 1 (GLP-1)Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Room Temp0.4 µMApr-24Human plasma proteases + DPP IVMS, ELISAEDTA plasmain vitroNoneNoneNot reported
2743
262221802015
HA/EGTFTSDVSSYLEGQAAKEFIAWLVKGR
G36A or [GLP-1(7-36A)]30FreeAmidationLinearLNoneGlucagon-like peptide 1 (GLP-1)Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)On ice0.4 µM12 ±3Human plasma proteases + DPP IVMS, ELISAEDTA plasmain vitroNoneNoneNot reported
2748
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 µM04 to 18Human plasma proteases + DPP IVMS, ELISAEDTA plasmain vitroNoneNoneNot reported
2753
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 µM12 ±1.0Human blood proteases + DPP IVMSP800 whole bloodin vitroNoneNoneNot reported
2755
262221802015
YA/EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ
GIP (1-42) (Glucosedependent insulinotropic polypeptide)42FreeFreeLinearLNoneProprotein of gastrointestinal tractAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Room Temp0.4 µMMay-20Human plasma proteases + DPP IVMSEDTA plasmain vitroNoneNoneNot reported
2756
262221802015
YA/EGTFISDYSIAMDKIHQQDFVNWLLAQKGKKNDWKHNITQ
GIP (1-42) (Glucosedependent insulinotropic polypeptide)42FreeFreeLinearLNoneProprotein of gastrointestinal tractAntihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner)Room Temp0.4 µMMay-20Human serum proteases + DPP IVMSSerumin vitroNoneNoneNot reported
2760
262221802015
HS/QGTFTSDYSKYLDSRRAQDFVQWLMNT
Glucagon29FreeFreeLinearLNonePeptide hormone of pancreaseRegulates hypoglycemiaRoom Temp0.4 µMMay-20Human plasma proteases + DPP IVMSEDTA plasmain vitroNoneNoneNot reported
2765
263080952015
HAEGTFTSDVSSYLEGQAAKEEFIIAWLVKGRG
Liraglutide31FreeFreeLinearLAcylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chainGlucagon-like peptide 1 (GLP-1) analogueUpregulates intracellular cAMP resulting in the release of insulinBlood sample collected after 1-96 hours after the injection of peptide5nmol/Kg14.4 hoursRat plasma proteasesELISA, LC/MSRat Plasma (Dose i/v injected)in vivoNoneNoneNot reported
2772
263372312015
MWQRPSSWIEGRLLTHTISRIAVSYQTKVNLL
RMP-16 (Recombinant slow-release TNF α-derived peptide)32FreeFreeLinearLNoneRecombinant slow-release TNF α-derived peptideTumor growth inhibitor and anti-angiogenicBlood sample collected after0.5-24 hours after the injection of peptide5mg/kg13.11 ±1.49BALB/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, the tumor inhibition rates of RMP16-treated mice was 78.11%
2783
256256502015
HAEGTFTSDVSSYLEGQAAK(γ-Glu-palmitoyl)EFIAWLVRGRG
Liraglutide31FreeFreeLinearLγ-Glu-palmitoyl at 21 st positionAnalog of human GLP-1GLP-1 receptor agonist0.25-84 hours0.6mg s/c injected12 ±2.8Cat blood proteasesELISAHealthy cat blood (Dose s/c injected)in vivoNoneNoneInsulin secretion increased 760.8 ± 350.7 (449 €“1,493) ng/L on Liraglutide administration as compared to normal 455.5 ±115.8 (411 €“660) in hyperglycemic patients
2796
241398442013
HSSKLQ
Conjuagte 2(conjugates of 4-aminocyclophosphamide (4-NH2-CPA))6SuccinylationAmidated CPALinearLNoneSynthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA)Anti-cancerNot mentionedNot mentioned12PSA(Prostate-specific antigen )HPLCConjuagte 2+PSA(Prostate-specific antigen)in vitroNoneNonepEC50-8.59 ±0.9minutes, Emax 9.30 ±0.26nmol/well
2814
50922902014
LLGDFFRKSKEKIGKEFKRIVQRIKDFLRNLVPRTES
LL-37 (Antimicrobial Peptide)37FreeFreeLinearLNoneHuman epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein)Antimicrobial15-720 minutes hour3 µM>12CathepsinProteolysis assay, (confirmed by Western blotting)Western Blottingin vitro16716248NoneNot reported
2821
13290461992
Pyr-QRLGNQWAVGHLL
[Psi13,14]BN [Bombesin antagonist]14FreeAmidationLinearLPyr=Pyro-glutamineBombesin analogueGrowth inhibitors0-1080 minutes50μM646Degradative enzymes or SCLC cell line proteasesRP-HPLCSCLC cell line NCI-H345in vitroNoneNoneIC50= 30nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line
2971
25562151989
DRVYIHPFHL
Angiotensin I (AI)10FreeFreeLinearLNoneDerived from angiotensinPrecusor of angiotensin- II (AII)37 °C100 - 2000 ng/ml12.6Fetal calf serum proteasesRadioimmunoassayPrimary endothelial cells + Fetal calf Serum (5%) + heat inactvationin vitroNoneNoneNot mentioned
2989
82172161993
SDKP
AcSDKP (Acetyl-SDKP)4AcetylationFreeLinearLNoneIsolated from fetal calf bone marrowNatural hemoregulatory37 °C for 24 hours4 X lO-7M, 10 µCi11.5Proteases from Heat inactivated calf serumHPLCHeat inactivated calf serum + 1μM catroprilin vitroNoneNoneNot reported
2994
82184821993
YRGDS
YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer)5FreeFreeLinearLPeptide covalently attached to Isocyanate containing polyurethane prepolymerSynthetic RGD containing peptideCell attachment propertyNot mentionedNot mentioned11.3(Half life of 2nd phase)Proteases from mouse boodHPLCMouse bloodin vivoNoneNoneNot reported
3121
212107102011
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCR
Linear chlorotoxin(CTX)36FreeFreeLinearLN-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 27Scorpion venomIdentify tumor foci with high sensitivity24 hours50μl of 40μM14Mice serum proteasesImaging system to measure fluorescent intensityIntravenous injection in two month old wild-type C57BL/6 micein vivohttp://www.drugbank.ca/drugs/DB00140NoneFluorescent efficiency (cm2) in the tumor compared with control mice=2.49 ±1
3122
212107102011
MCMPCFTTDHQMARKCDDCCGGKGRGKCYGPQCLCRGAGAAGG
Cyclic chlorotoxin(CTX)43FreeFreeCyclic (C2-C19, C5-C28, C16-C33, C20-C35)LN-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 28Analog of CTXIdentify tumor foci with high sensitivity24 hours50μl of 40μM11Mice serum proteasesImaging system to measure fluorescent intensityIntravenous injection in two month old wild-type C57BL/6 micein vivohttp://www.drugbank.ca/drugs/DB00141NoneFluorescent efficiency (cm2) in the tumor compared with control mice=3.3 ±1.81
4009
387890612024
HAEGTFTSDVSSYLEGQAAKEFIAWLVKGRG
Liraglutide (Lymph cannulated)31FreeFreeLinearLLys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGluGLP-1 analogsAntidiabetesLymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr2 mg/kg12.61 ± 5.45 Male SD rats lymph proteaseUHPLCMale SD rats thoraic lymphIn VivoNoneNoneN.A.
4010
387890612024
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide (Lymph cannulated)39FreeAmidationLinearLNoneExendin-4 analogsAntidiabetesLymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr1 mg/kg10.26 ± 6.51 Male SD rats lymph proteaseUHPLCMale SD rats thoraic lymphIn VivoPDB id: 7MLLNoneN.A.
4055
383407262024
IEEQAKTFLDKFNHEAEDLFYQSSLGGSKGDFRGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSGGGGSDVDLGDISGINASVVNIQKEIDRLNEVAKNLNESLIDLQELGKYEQ
A1L35HR2m-Chol114Conjugation of angiotensin-converting enzyme 2 (ACE2)-derived peptide A1 to the N terminus of the viral HR2-derived peptide HR2m through a long flexible linker,Chol conjugation at C terminalLinearLNonefusion protein of A1 and HR2mAntiviral (Inhibits Coronaviruses)N.A.5 mg/kg10.6Balb/c mice serum proteaseN.A.Balb/c mice trachea tissue homogenate In VivoNoneNoneA1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM
4058
382935402024
ENLYFQHGEGTFTSDVSSYLEGQAAKEFIAWLVKGRGGGGSGGGGSGGGGSLAEAKVLANRELDKYGVSDYYKNLINNAKTVEGVKALIDEILAALPGGGGSGGGGSGGGGSHSQGTFTSDYSKYLDSRRAQDFVQWLMNTGGEGGSEGSEGEGSEGSGEGEGGSEGSEGEGSEGSGEGEGGSEGSEGEGGSEGSEGEGGEGSGEGEGSEGSGEGEGSGEGSEGEGGSEGGEGEGSEGGSEGEGSEGGSEGEGGEGSGEGEGGGEGSEGEGSEGSGEGEGSGEGSEG
GLP-ABD-XTEN144257GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tagABD was connected to the N-terminus of the XTEN polypeptide (144 amino acids) through a (GGGGS)3 linkerLinearLNoneFusion protein of GLP-1, ABD, XTEN (either 144 or 288)Antidiabetes, AntiobesityAt 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein5 nmol12.9C57Bl/6 mice plasma protease And DPP-4ELISAC57BL/6 mice plasmaIn VivoNoneNoneGLP-ABD-XTEN144 has a Kd value of only 5.50 nM
4060
382365612024
HQGTFTSDKSEYLDSERARDFVAWLEAGG
Cotadutide29FreeFreeLinearLpalm-Glu-OH conjugated at Lys9 side chainSyntheticDual GLP-1 and Glucagon (GCG) Receptor agonist N.A.20 to 600 μg13.3N.A.N.A.N.A.In VivoNoneNoneN.A.
4186
374497812023
pSar200-b-pCys(SO2Et)30
NCL30230Polysarcosine = poly(N-methyl glycine)FreeLinearLfluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine)syntheticImprove the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formationBlood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h5 μg/μL11.4C57BL/6 mice plasma proteaseFluorescence spectrophotometryC57BL/6 mice plasma In VivoNoneNoneNot mentioned
4187
374497812023
pSar200-b-pCys(SO2Et)30
2F-CL30230Polysarcosine = poly(N-methyl glycine)FreeLinearLfluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine)syntheticImprove the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formationBlood samples of 50 μL were collected from the tail vein at the defined time points after systemic administration: 10 min, 1 h, 6 h, 24 h, 72 h5 μg/μL11.3C57BL/6 mice plasma proteaseFluorescence spectrophotometryC57BL/6 mice plasma In VivoNoneNoneNot mentioned
4262
366319712023
LVPRVDKPPYLPRPRPPROIYNO
20k-prodrug23Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGsAmidation, Orn at position 23LinearLOrn at postion 19SyntheticAntimicrobial0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates31.5 μmol/L14Mouse serum proteaseSerum stability assayMouse serumIn VivoNoneNone20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines
4268
366308262023
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Ex-PEGRh(4.4 ± 1.1nm)39FreePEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCOLinearLFluorescently labeledExendin-4 analogsAntidiabetesBlood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h1000 nmol kg−111.9 ± 2.7 (T1/2 Elimination)Immunized mice plasma proteaseFluorescence assayImmunized mice plasmaIn VivoNoneNoneEC50 = 1.3 ± 0.2 nM
4269
366308262023
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Ex-POEGMAopt(54.7KDa)39FreePOEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa)LinearLFluorescently labeledExendin-4 analogsAntidiabetesBlood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h1000 nmol kg−112.1 ± 1.0 (T1/2 Elimination)Immunized mice plasma proteaseFluorescence assayImmunized mice plasmaIn VivoNoneNoneEC50 = 2.8 ± 0.7 nM
4280
366308262023
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Ex-PEGRh 39Fluorescently labelledExendin-DBCO was conjugated to azide-functional PEG(27.7KDa)LinearLNoneExendin-4 analogsAntidiabetesTen μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. 1000 nmol/kg11.9 ± 2.7 (T1/2 Elimination) Immunized mice plasma proteasefluorescence assayImmunized mice plasmaIn VivoNoneNoneEC50 (nM) = 1.3 ± 0.2
4287
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KEEIHQ-Aib-EFIEWLLAQGPSSGAPPPS
SEQ ID NO 1939FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application0.5 mg/kg10.3Mice plasma proteaseLC-MSMice plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 2.0
4290
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KDRIHQ-Aib-EFIEWLLAQRG
SEQ ID NO 631FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application0.25 mg/kg11.2Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.5
4292
N.A.2023
Y-Aib-EGT-Iva-ISDLSI-Aib-KDRIHQ-Aib-EFIEWLLAQRG
SEQ ID NO 1631FreeAmidationLinearLAib = α-aminoisobutyric acid, Iva = IsovalineExendin-4 analogsAntidiabetesBlood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application0.25 mg/kg11.5Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.1
4293
N.A.2023
Y-Aib-EGT-Iva-ISDLSI-Aib-KDRIHQ-Aib-EFIEWLLAQRG
SEQ ID NO 1631FreeAmidationLinearLAib = α-aminoisobutyric acid, Iva = IsovalineExendin-4 analogsAntidiabetesBlood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application0.5 mg/kg10.8Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.1
4296
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KERIHQ-Aib-EFIEWLLAQGPSSGAPPPS
SEQ ID NO 2139FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application0.25 mg/kg12.9Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.8
4297
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KERIHQ-Aib-EFIEWLLAQGPSSGAPPPS
SEQ ID NO 2139FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application0.5 mg/kg12.1Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.8
4298
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KDR-Aib-HQ-Aib-EFIEWLLAQRPSSGAPPPS
SEQ ID NO 2239FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application0.25 mg/kg13.6Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 1
4300
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KDRIHQEEFIQWLLAQGPSSGAPPPS
SEQ ID NO 3539FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application0.25 mg/kg14.5Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.6
4301
N.A.2023
Y-Aib-EGTFISDLSI-Aib-KDRIHQEEFIQWLLAQGPSSGAPPPS
SEQ ID NO 3539FreeAmidationLinearLAib = α-aminoisobutyric acidExendin-4 analogsAntidiabetesBlood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application0.5 mg/kg14.3Rats plasma proteaseLC-MSRats plasmaIn VivoNoneEP 2022074607 WIC50 hGIPR (nM) = 0.6
4315
N.A.2023
PXXFLSPYHSRVSSRKESKKPPAKLSPRK
SEQ ID NO 3129FreeFreeLinearLX = Octanoyl-Dpr at position 3, NMeS = N- methyl-L-serine at position 2Human Ghrelin AnalogGhrelin Receptor AgonistSolutions were incubated at 37 C for 60, 120 and 180 Minutes1 mg/ml12Plasma proteaseLC-MSDiluted plasma In VitroNoneEP 2023054305 WEC50(nM) = 50.3
4468
363809172022
HAEGTFTSNVSSYLEGQAAKEFIAWLVKGRG
Glycan-GLP-1-1(G2S2)31FreeFreeLinearLN-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan)GLP-1 analogsAntidiabetes37 °C6 nmol736.6 ± 12.3Mouse serum proteaseRP-HPLCMouse serumIn VitroNoneNoneBGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) 
4470
363809172022
HAEGTFTSDVSSYLEGQAANESIAWLVKGRG
Glycan-GLP-1-3(G2)31FreeFreeLinearLN-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan)GLP-1 analogsAntidiabetes37 °C6 nmol738.6 ± 9.7Mouse serum proteaseRP-HPLCMouse serumIn VitroNoneNoneBGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) 
4476
363809172022
HAEGTFTSDVSSYLEGQAAKEFIAWLVNGTG
Glycan-GLP-1-5(G2S2) 31FreeFreeLinearLN-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan)GLP-1 analogsAntidiabetes37 °C6 nmol777.0 ± 10.2Mouse serum proteaseRP-HPLCMouse serumIn VitroNoneNoneBGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) 
4486
363239882022
HADGSFSDEMNTILDNLAARDFINWLIQTKITD
Glepaglutide 33FreeFreeLinearLNoneGLP-2 analogueTreatment of Short Bowel Syndrome Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 221 mg10.4Human plasma proteaseLC-MSHuman plasmaIn VivoNoneNoneEC50 = 0.12 nM In vitro potency
4487
363239882022
HGEGTFSSELATILDALAARDFIAWLIATKITDKKKKKK
Glepaglutide parent39FreeSix lysines has been added at C terminal , AmidationLinearLNoneGLP-2 analogueTreatment of Short Bowel Syndrome Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 221 mg11.7Human plasma proteaseLC-MSHuman plasmaIn VivoNoneNoneEC50 = 0.12 nM In vitro potency
4494
361427492022
Dmt-kFFKKPFTL
PK2010Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1FreeLinearMixD-amino acid residue (D-Lys) inserted at position 2opioid–neurotensin hybrid peptideAnalgesic 37°C for 24 h50 μg/mL11.36N.A.LC-MS1M NaOHIn VitroNoneNoneEC50 = 79 nM (potency at mu opioid receptor)
4520
360758992022
N.A.
S-20-1N.A.N.A.N.A.CyclicLModified by adding negative chargeSyntheticAntiviral (Against Infection By Sars-Cov-2 )Blood samples were collected at 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h and 48 h50 mg/kg14.53 (Terminal Elimination Half Life)C57Bl/6 mice plasma proteaseLC-MS/MSC57BL/6 mice plasmaIn VivoNoneNoneIC50 (μM) = 0.8 in HUH 7 cells
4527
359900072022
desH-AEGTFTSDVSSYLEEQAAREFIAWLVRGRKX
Peptides 131desH indicates the non-natural amino acid deamino-histidineFreeLinearLX = R1, R2 = H (R2 group present in R1)GLP-1R agonistAntidiabetes, Antiobesity200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h20 nmol/kg10.9Rats plasma proteaseUPLC-MSRats plasmaIn VivoNoneNoneN.A.
4528
359900072022
desH-AEGTFTSDVSSYLEEQAAREFIAWLVRGRKX
Peptides 131desH indicates the non-natural amino acid deamino-histidineFreeLinearLX = R1, R2 = H (R2 group present in R1)GLP-1R agonistAntidiabetes, Antiobesity200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h18059 pmol/kg12.2Rats plasma proteaseUPLC-MSRats plasmaIn VivoNoneNoneN.A.
4529
359900072022
desH-AEGTFTSDVSSYLEEQAAREFIAWLVRGRKX
Peptides 131desH indicates the non-natural amino acid deamino-histidineFreeLinearLX = R1, R2 = H (R2 group present in R1)GLP-1R agonistAntidiabetes, Antiobesity200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h18058 pmol/kg10.7Rats plasma proteaseUPLC-MSRats plasmaIn VivoNoneNoneN.A.
4531
359900072022
desH-AEGTFTSDVSSYLEEQAAREFIAWLVRGRKX
Peptides 131desH indicates the non-natural amino acid deamino-histidineFreeLinearLX = R1, R2 = H (R2 group present in R1)GLP-1R agonistAntidiabetes, Antiobesity200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h18052 pmol/kg12.9Rats plasma proteaseUPLC-MSRats plasmaIn VivoNoneNoneN.A.
4544
358922562022
GIVEQCCTSICSLYQLENYCN/FVNQHLCGSHLVEALYLVCGERGFFYTPKT
RA1512734351FreeFreeLinearLAlbumin binding fatty-acid side chain is coupled to lysine (B29)Insulin analogueAntidiabetesN.A.200 nmol/kg11Rats plasma proteaseLC-MS/MSRats plasmaIn Vivohttps://sci-hub.st/10.1016/j.jpba.2018.07.009None(Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM
4593
356884762022
DNPSLSIDLTFHLLRTLLELEKQEKEKQQACQNRIIFDSV
PEG-hUCN140FreeAmidationLinearLInsertion of a cysteine residue at position 31 for pegylation PEG20 acetamideHuman UCN1 derivativeTreating Autoimmune diseaseN.A.0.3 mg/kg13C57Bl/6J mice plasma proteaseLaser capture/mass spectrometryC57BL/6J mice plasmaIn VivoNoneNoneAt the CRHR1 receptor, the PEG-hUCN1 peptide was less potent than native CRH or UCN1 peptides with EC50 values of 47, 15, and 10 nM, respectively
4596
356773072022
MTPLGPASSLPQSFLLKCLEQVRKIQADGAALLANQVRQVGDGAALQEKLVSELGNALENALPDTLDTLQLDVKDYFSLRAALLAALPTRLRYLQEADAFQRRAGGVLVASHLGTSLQRLALADSGVLRQLLYYIESGPHQAPLGTGGADQGAMNVTCSKELQAYREQILHDCWLPKDLKDLQLLIEMNVTVLVDIDKLVEVLRLRQGVLHGVHVC
PEG10k-rhG-CSF175FreeFreeLinearLPEG10K-MAL fatty chain-modification of rhG-CSF at Cys18 positionrhG-CSF derivativeN.A.sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168h1.0 mg/kg13.05 ± 0.45Mice Serum ProteaseELISAMice serum In VivoNoneNoneN.A.
4614
355828522022
lKlW
CP8FreePNAM37 linked through NH2 groupCyclic(N-C terminal bond)MixD-leucine at position 1 and 3SyntheticDrug delivery vectorsBlood samples (0.2 mL) were taken prior to dose administration and at 1, 5, 10, 20, 30, 60, 120, 180, 240, 360, 480, and 1440 min after dose administratio1 μCi14.6 ± 2.9 (Elimination Half Life)Rats plasma proteaseLiquid scintillation counterRats plasmaIn VivoNoneNoneFor concentrations of 1 mg/mL CP , cell viabilities drop to about 75% for the 4T1 cell line
4634
354148772022
MCFTHFHMLWPFCGSGSDYKDDDDK
B_1275.125C18 diacid-gGlu-2xOEGAmidation, FLAG tagCyclicLNoneSyntheticTargets GIP receptorN.A.2 μM643(Elimination Half Life)Rats plasma proteaseLC-MSRats plasmaIn VivoNoneNoneIC50(nM) = 1209
4682
348077602022
RRWVRRVRRVWRRVVRVVRRWVRR
PLG020624FreeFreeLinearLNoneSyntheticAntimicrobialBlood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion0.125 mg/kg10.5 (Median Terminal Half Life)Human plasma protease HPLC-MSHuman plasmaIn VivoPubchem CID : 16152467NoneN.A.
4684
348077602022
RRWVRRVRRVWRRVVRVVRRWVRR
PLG020624FreeFreeLinearLNoneSyntheticAntimicrobialBlood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion0.25 mg/kg13.16 (Median Terminal Half Life)Human plasma protease HPLC-MSHuman plasmaIn VivoPubchem CID : 16152467NoneN.A.
4782
351779452022
QRPRLSHKGPMPA
(Ala13)apelin-1313FreeAla13 modifcation, carboxylationLinearLNoneApelin-13 AnalogueInsulinotrophic activity0, 2, 4, 8, 24 h20 μg 10.3Mouse plasma proteaseRP-HPLCMouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer In Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneEC50(M) = 1.74e-009 (In vitro insulin secretion)
4784
351779452022
pGlu-RPRLSHKGPMPA
pGlu(Ala13)apelin-1313pGlu = PyroglutamateAla13 modifcation, carboxylationLinearLNoneApelin-13 AnalogueInsulinotrophic activity0, 2, 4, 8, 24 h20 μg 11.1Mouse plasma proteaseRP-HPLCMouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer In Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneEC50(M) = 7.68e-009 (In vitro insulin secretion)
4786
351779452022
pGlu-RPRLSHKGPMPY
pGlu(Tyr13)apelin-1313pGlu = PyroglutamateTyr13 modifcation, carboxylationLinearLNoneApelin-13 AnalogueInsulinotrophic Activity0, 2, 4, 8, 24 h20 microgram12.2Mouse plasma proteaseRP-HPLCMouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer In Vitrohttps://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/NoneEC50(M) = 1.48e-008 (In vitro insulin secretion)
4798
352591492022
(CH-Mal-C6-GIVEQCCTSICSLYQLENYCN)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C6-Mal-CH)
CH-/HPN-Conjugated Insulins (GlyA1/LysB29)50Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH]K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH]Cyclic (C6-C11 disulfide bond in A chain)LC7-C7 and C20-C19 disulfide bond between A and B chainHuman insulin analogAntidiabetesBlood samples were collected immediately before injection and at various time points up to 48 h after injection340 nmol/kg11.8Mice serum proteaseSandwich ELISAMice serumIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneEC50(nM) = 32.87
4803
352591492022
(CH-Mal-C11-GIVEQCCTSICSLYQLENYCN)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C11-Mal-CH)
CH-/HPN-Conjugated Insulins (GlyA1/LysB29)50Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]Cyclic (C6-C11 disulfide bond in A chain)LC7-C7 and C20-C19 disulfide bond between A and B chainHuman insulin analogAntidiabetesBlood samples were collected immediately before injection and at various time points up to 48 h after injection340 nmol/kg14Mice serum proteaseSandwich ELISAMice serumIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneEC50(nM) = 86.25
4804
352591492022
(CH-Mal-C11-GIVEQCCTSICSLYQLENYCN)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C11-Mal-CH)
CH-/HPN-Conjugated Insulins (GlyA1/LysB29)50Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH]Cyclic (C6-C11 disulfide bond in A chain)LC7-C7 and C20-C19 disulfide bond between A and B chainHuman insulin analogAntidiabetesBlood samples were collected immediately before injection and at various time points up to 48 h after injection340 nmol/kg12.1Mice serum proteaseSandwich ELISAMice serumIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneEC50(nM) = 86.25
4810
352591492022
(HPN-Mal-C11-GIVEQCCTSICSLYQLENYCN)-(FVNQHLCGSHLVEALYLVCGERGFFYTPK-C11-Mal-HPN)
CH-/HPN-Conjugated Insulins (GlyA1/LysB29)50Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN]K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN]Cyclic (C6-C11 disulfide bond in A chain)LC7-C7 and C20-C19 disulfide bond between A and B chainHuman insulin analogAntidiabetesBlood samples were collected immediately before injection and at various time points up to 48 h after injection100 nmol/kg12.9Mice serum proteaseSandwich ELISAMice serumIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneEC50(nM) = 88.23
4814
352591492022
(HPN-Mal-C3-GIVEQCCTSICSLYQLENYCN)-FVNQHLCGSHLVEALYLVCGERGFFYTPK
CH-/HPN-Conjugated Insulins (GlyA1)50Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN]FreeCyclic (C6-C11 disulfide bond in A chain)LC7-C7 and C20-C19 disulfide bond between A and B chainHuman insulin analogAntidiabetesBlood samples were collected immediately before injection and at various time points up to 48 h after injection100 nmol/kg11.7Mice serum proteaseSandwich ELISAMice serumIn Vivohttps://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/NoneEC50(nM) = 6.54
4834
358075582022
IKPEAPGEDASPEELNRYYASLRHYLNLVTR-MeArg-Y
[MeArg35]PYY3−3634FreeMethylated Arg35 at C terminusLinearLNonePYY analogueAntidiabetes, AntiobesityThe reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)1 μM620Minipigs plasma proteaseLC-MSMinipigs plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/NoneKi(nM) = 500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4835
358075582022
IKPEAPGEDASPEELNRYYASLRHYLNLVTR-MeGln-RY
[MeGln34]PYY3−3634FreeMethylated Gln34 at C terminusLinearLMethylated Gln34PYY analogueAntidiabetes, AntiobesityThe reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)1 μM890Minipigs plasma proteaseLC-MSMinipigs plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/NoneKi(nM) = 0.40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4838
358075582022
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQ-βArg-Y
[β-homoArg35]PYY3−3634Freeβ-homoArg35 at C terminusLinearLNonePYY analogueAntidiabetes, AntiobesityThe reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min)1 μM680Minipigs plasma proteaseLC-MSMinipigs plasmaIn Vitrohttps://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/NoneKi(nM) = 6300 (In Vitro Binding of Peptide Analogues against Human Y1 receptor)
4858
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 234FreeAmidationLinearLFatty acid conjugation at position 4 (C18 diacid-γGlu-2xAdo)Derived from PYYAntiobesityBlood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing15 nmol/kg14Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneEC50(nM) = 10 for Y2 receptor
4860
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 734FreeAmidationLinearLFatty acid conjugation at position 9Derived from PYYAntiobesityN.A.15 nmol/kg12Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneEC50(nM) = 40 for Y2 receptor
4862
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 934FreeAmidationLinearLFatty acid conjugation at position 11Derived from PYYAntiobesityN.A.15 nmol/kg11Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneEC50(nM) = 1.3 for Y2 receptor
4863
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 1134FreeAmidationLinearLFatty acid conjugation at position 13Derived from PYYAntiobesityN.A.15 nmol/kg13Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneEC50(nM) = 16 for Y2 receptor
4875
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNLVTRQRY
PYY3-36 analogues 3934FreeAmidationLinearLFatty acid conjugation at position 30Derived from PYYAntiobesityN.A.15 nmol/kg13Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneN.A.
4886
347071782021
IKPEAPGEDASPEELNRYYASLRHYLNRKVTRQRY
PYY3-36 analogues 5035FreeAmidationLinearLFatty acid conjugation at position 30, Acetylation at Asn28Derived from PYYAntiobesityN.A.15 nmol/kg120Male göttingen minipigs plasma proteaseLC-MSMale göttingen minipigs plasma In VivoNoneNoneN.A.
4920
341633522021
NMP-YKEIEQLIELANYQV
NOPT16OPT substituted with an N-methyl proline at position 1FreeLinearLNoneDerived from OPTBinds To Pser68-PlmAliquots of 50 μl were collected at different time points (0–48 h)300 μM14.9Human serum proteaseMass spectrometryHuman serum In VitroNoneNoneN.A.
4934
339400582021
gqsehhmrvysf
OPBP-1@TMC12FreeFreeLinearDSubstituition 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.20 mg/kg14.55 ± 1.43Male 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.
4936
339188532021
TSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIKKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLG-GGGSGGGTGGGSGGG-GFLG-ASPAAPAPAPAAPAPSAPAASPAAPAPASPAAPAPSAPA-GGSGG
HFn-PAS/DOX235Free15aa linker, enzyme cleavable site, PAS(40), 5 aa flexible linker conjugated at C terminus LinearLNoneSyntheticAntitumorBlood samples were collected from the retro orbital sinus at fixed time points (10, 30 min, 1, 2, 4, 8, 12, 24, 36, 48 h) at 37 °C3.0 mg/kg14.96 ± 0.29SD rats serum proteaseFluorescence spectrometrySD rats serumIn VivoPDB id: 3AJONoneIC50 (μg mL−1) = 0.38 ± 0.09
5038
320786722020
KTRHYFIAAVERLWDYGMSSSPHVLRNRAQSGSVPQFKKVVFQEFTDGSFTQPLYRGELNEHLGLLGPYIRAEVEDNIMVTFRNQASRPYSFYSSLISYEEDQRQGAEPRKNFVKPNETKTYFWKVQHHMAPTKDEFDCKAWAYFSDVDLEKDVHSGLIGPLLVCHTNTLNPAHGRQVTVQEFALFFTIFDETKSWYFTENMERNCRAPCNIQMEDPTFKENYRFHAINGYIMDTLPGLVMAQDQRIRWYLLSMGSNENIHSIHFSGHVFTVRKKEEYKMALYNLYPGVFETVEMLPSKAGIWRVECLIGEHLHAGMSTLFLVYSNKCQTPLGMASGHIRDFQITASGQYGQWAPKLARLHYSGSINAWSTKEPFSWIKVDLLAPMIIHGIKTQGARQKFSSLYISQFIIMYSLDGKKWQTYRGNSTGTLMVFFGNVDSSGIKHNIFNPPIIARYIRLHPTHYSIRSTLRMELMGCDLNSCSMPLGMESKAISDAQITASSYFTNMFATWSPSKARLHLQGRSNAWRPQVNNPKEWLQVDFQKTMKVTGVTTQGVKSLLTSMYVKEFLISSSQDGHQWTLFFQNGKVKVFQGNQDSFTPVVNSLDPPLLTRYLRIHPQSWVHQIALRMEVLGCEAQDLYDKTHTCPPCPAPELLGGPSVFLFPPKPKDTLMISRTPEVTCVVVDVSHEDPEVKFNWYVDGVEVHNAKTKPREEQYNSTYRVVSVLTVLHQDWLNGKEYKCKVSNKALPAPIEKTISKAKGQPREPQVYTLPPSRDELTKNQVSLTCLVKGFYPSDIAVEWESNGQPENNYKTTPPVLDSDGSFFLYSKLTVDKSRWQQGNVFSCSVMHEALHNHYTQKSLSLSPG
rFVIIIFc865FreeIgG1 FcLinearLNoneSyntheticRole In ClottingN.A.200 IU/kg13.2VWF Het mice plasma proteasechromogenic activity assaysVWF Het 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
5095
328581242020
C13-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip
Cmpd# 1016Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13FreeLinearMixhArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acidDerived from pyr-apelin-13Treatment of Chronic Hepatic FailureN.A.0.5 mg/kg10.2Male SD rats plasma proteaseScintillation proximity assayMale SD rats plasmaIn VivoNoneNoneRat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6
5097
328581242020
C17-γGlu-OEG-OEG-hArg-rQ-hArg-Pr-NMeLeu-SHKG-Oic-pIPhe-P-DBip
Cmpd# 1416Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17FreeLinearMixhArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid Derived from pyr-apelin-13Treatment of Chronic Hepatic FailureN.A.0.5 mg/kg10.3Male SD rats plasma proteaseScintillation proximity assayMale SD rats plasmaIn VivoNoneNoneRat GTPγS (nM) EC50 ± SE =7.42 ± 0.9
5115
328030732020
GSLTSSERIDKQIRYILDGISALRKETCNKSNMCESSKEALAENNLNLPKMAEKDGCFQSGFNEETCLVKIITGLLEFEVYLEYLQNRFESSEEQARAVQMSTKVLIQFLQKKAKNL-AzF-AITTPDPTTNASLLTKLQAQNQWLQDMTTHLILRSFKEFLQSSLRALRQM
Pal-Rb169FreeFreeLinearLConjugation of palmitic acid at AzF, biotinylated labelling, , (AzF) was incorporated into the position 126 on the repebody followed by lipid conjugationSyntheticAntitumorBlood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h10 mg/kg10.7 (Elimination 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.
5127
326081852020
GGRSFFLLRRIQGCRFRNTVDDY
125I-M-E522FreeTyrosine (Y) residue was added to E5 sequence and 125I was addedLinearLNoneSyntheticAnticancer (Treatment of Acute Myeloid Leukemia) N.A.50 µg/g14.53 ± 6.04Rats plasma proteaseGamma counterRats plasmaIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC4196105/#sec10NoneThe cells that were pretreated with M-E5 showed significantly reduced migration compared with the CXCL12 group, and the inhibitory rate was 82.9% for the leukemic cells separated from the spleen and 59.1% for those separated from the BM
5161
324045232020
WMEWDREINNYTSLIHSLIEESQNQQEKNEQELL
PEG40-NC34FreeFreeLinearLPEGylation at Asn637 in native gp41Derived 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/kg10.39Rats plasma proteaseHIV inhibition assayRats plasmaIn VivoNoneNone[EC50] = 18.51 nM for PEG40-NC (antiviral activity)
5189
354966222020
HGEGTFTSDLSQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKKK
Lixisenatide 1a 44FreeAmidationLinearL(X1) MPAs modification on Lys12 lixisenatide analoguesAntidiabetesincubated at 37 °C for 6, 12, 24, and 48 h1000 ng/mL13.2Rats blood plasma proteaseLC-MS/MSRats blood plasma In VitroNoneNoneEC50(nM) = 0.19 ± 0.02 for Lixisenatide 1a (in vitro GLP-1 receptor activation potency)
5192
354966222020
HGEGTFTSDLSKQMEEEAVRLFIEWLNGGPSSGAPPSKKKKKK
Lixisenatide 1d44FreeAmidationLinearL(X1) MPAs modification on Lys12 lixisenatide analoguesAntidiabetesincubated at 37 °C for 6, 12, 24, and 48 h1000 ng/mL13.1Rats blood plasma proteaseLC-MS/MSRats blood plasma In VitroNoneNoneEC50(nM) = 0.085 ± 0.021 for Lixisenatide 1d (in vitro GLP-1 receptor activation potency)
5195
354966222020
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPSKKKKK
Lixisenatide 1g44FreeAmidationLinearL(X1) MPAs modification on Lys12 lixisenatide analoguesAntidiabetesincubated at 37 °C for 6, 12, 24, and 48 h1000 ng/mL11.9Rats blood plasma proteaseLC-MS/MSRats blood plasma In VitroNoneNoneEC50(nM) = 0.59 ± 0.16 for Lixisenatide 1g (in vitro GLP-1 receptor activation potency)
5203
321333412020
CNCKAPETARCAIRCVIFTSGGSRW
Apamin based analogs 325FreeFreeCyclic (C1-C11, C3-C15)LNoneApamin based analogs Roles in metabolism, arousal, learning and memoryN.A.0.05 μg/μl12.8Human serum proteaseLC-MSHuman serumIn VitroNoneNoneBinding affinity pKi ± SEM [logM] = 6.65 ± 0.18 
5218
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 injection0.025 mg/kg782 ± 365 (Elimination Half Life)Göttingen minipigs plasma proteaseLC-MS/MSGöttingen minipigs plasmaIn VivoNoneNoneEC50(nM) = 0.24 for hGLP-2 receptor
5221
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 169 h post injection1 mg/kg11.7 ± 1.4 (Terminal Half Life)Rats plasma proteaseLC-MS/MSRats plasma In VivoNoneNoneEC50(nM) = 0.24 for hGLP-2 receptor
5268
N.A.2020
CSWPA-hArg-CLHQDLC
Ac-(06-34-18) (HomoArg5)12AcetylationFreeLinearLHomoArg6 replaces Arg (R) SyntheticTargets plasma kallikreinN.A.5 uM10.7Rats plasma proteaseWaters Xevo TQ-MSRats plasmaIn VitroNoneUS 201214350192 AIC50(nM)(rat kallikrein) = 64
5275
N.A.2020
CSFPY-hArg-CLHQDLC
Ac-(06-34-18) Phe2 Tyr4 HomoArg512AcetylationFreeLinearLHomoArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with TyrSyntheticTargets plasma kallikreinN.A.5 uM12.2Rats plasma proteaseWaters Xevo TQ-MSRats plasmaIn VitroNoneUS 201214350192 AIC50(nM)(rat kallikrein) = 19.7
5311
316546852019
HGEGTFTSDVSSYLEGQAAKEFIAWLVKGRAEAAAAKEAAAAKEAAAAKA
Repebody-fused GLP-1 in complex with HSA50RepebodyGLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminusLinearLNoneSyntheticAntidiabetesMice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis25 nmol/kg10.7 (Terminal Half Life) Mice plasma proteaseSandwich ELISAMice plasmaIn VivoPDB id: 5VAINoneC57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases
5326
314431812019
MGVPRPQPWALGLLLFLLPGSLGAESHLSLLYHLTAVSSPAPGTPAFWVSGWLGPQQYLSYNSLRGEAEPCGAWVWENQVSWYWEKETTDLRIKEKLFLEAFKALGGKGPYTLQGLLGCELGPDNTSVPTAKFALNGEEFMNFDLKQGTWGGDWPEALAISQRWQQQDKAANKELTFLLFSCPHRLREHLERGRGNLEWKEPPSMRLKARPSSPGFSVLTCSAFSFYPPELQLRFLRNGLAAGTGQGDFGPNSDGSFHASSSLTVKSGDEHHYCCIVQHAGLAQPLRVELESPAKSSVLVVGIVIGVLLLTAAAVGGALLWRRMRSGLPAPWISLRGDDTGVLLPTPGEAQDADLKDVNVIPATA
FcRn365FreeFreeLinearLNoneIsolated from human gastric juiceRole in extending the serum half life of therapeutic antibodiesBlood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrsN.A.10.6PBMC lysate protease (African American)LC-MS/MSPBMC lysate (African American)In VitroUniprot id: P55899NoneN.A.
5327
314431812019
MGVPRPQPWALGLLLFLLPGSLGAESHLSLLYHLTAVSSPAPGTPAFWVSGWLGPQQYLSYNSLRGEAEPCGAWVWENQVSWYWEKETTDLRIKEKLFLEAFKALGGKGPYTLQGLLGCELGPDNTSVPTAKFALNGEEFMNFDLKQGTWGGDWPEALAISQRWQQQDKAANKELTFLLFSCPHRLREHLERGRGNLEWKEPPSMRLKARPSSPGFSVLTCSAFSFYPPELQLRFLRNGLAAGTGQGDFGPNSDGSFHASSSLTVKSGDEHHYCCIVQHAGLAQPLRVELESPAKSSVLVVGIVIGVLLLTAAAVGGALLWRRMRSGLPAPWISLRGDDTGVLLPTPGEAQDADLKDVNVIPATA
FcRn365FreeFreeLinearLNoneIsolated from human gastric juiceRole in extending the serum half life of therapeutic antibodiesBlood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrsN.A.11.6PBMC lysate protease (African American)LC-MS/MSPBMC lysate (African American)In VitroUniprot id: P55899NoneN.A.
5338
314532572019
N.A.
Pept. AN.A.FreeFreeCyclicLN.A.N.A.Therapeutic agent against a CNS-related disorderBlood (100 µl) and CSF (100 µl) aliquots for drug concentration assessment were collected pre-dose, on study day 1 at 0.5, 1.5, 3, 6, and 24 h post first dose, and on study day 2 at 1.5 h post the second dose (corresponding to 25.5 h from study start)4.2 mg/kg14.3 ± 5.5 (Terminal Half Life)göttingen Minipig Csf Lumbar ProteaseLC-MS/MSGöttingen minipigs CSF lumbarIn VivoNoneNoneN.A.
5358
312355322019
LQEHPNARKYKGANKKGLSKGCFGLKLDRIGSMSGLGC 
CNP-3838FreeFreeCyclic (1 Disulfide Bond)LNoneCNP-38 analogTreatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias4 days100 μg/ml12.6 ± 3.9 Recombinant human NEP proteaseHPLC-UVRecombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4)In VitroNoneNoneRatio IC50 CNP-38/IC50 CNP-38 conjugate = 100 (NPR-C Affinity)
5364
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/kg12.9 ± 4.6 Sham rats plasma proteaseLC–MS/MSSham rats plasmaIn VivoNoneNoneN.A.
5372
311560412019
LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK
AD-114-Im7 PEG 30K 118Freelm7-PEG30KLinearLNoneFusion protein of AD-114 with lm7Attenuates Renal fibrosis through blockade Of CXCRBlood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing3 mg/kg11.85Mouse plasma proteaseLC–MS/MSMouse plasmaIn VivoPDB id: >5AEA_1NoneKd(nM) = 0.7 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K 
5376
311560412019
LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK
AD-114-PA600-6H 118FreePA-600-6HLinearLNoneFusion protein of AD-114 with PA600Attenuates Renal fibrosis through blockade Of CXCRBlood samples were collected at 15, 30 min, 1, 2, 3, 4, 8, 12,18, 24, 36, 48 and 72 h post dosing10 mg/kg10.25Mouse plasma proteaseELISAMouse plasmaIn VivoPDB id: >5AEA_1NoneKd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K 
5380
311560412019
LQVDIVPSQGEISVGESKFFLCQVAGDAKDKDISWFSPNGEKLTPNQQRISVVWNDDSSSTLTIYNANIDDAGIYKCVVTGEDGSESEATVNVKIFQAAADYKDDDDKAADYKDDDDK
AD-114-PA600 118FreePA-600LinearLNoneFusion protein of AD-114 with PA600Attenuates Renal fibrosis through blockade Of CXCRBlood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. 3 mg/kg10.2 ± 3.9Cynomolgus monkeys plasma proteaseLC–MS/MSCynomolgus monkeys plasma dosed at Day 1In VivoPDB id: >5AEA_1NoneKd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K 
5394
310837402019
HSEGTFTSDVSSYLEGQAAKEFIAWLVKGGVKALIDEILAA
SKL-1828741FreeAmidationLinearL3H labeling at Tyr, Ser8 modificationGLP-1 analogsAntidiabetesBlood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration17.4 µ/kg11.4 ± 1.0 (Elimination Half Life)Cynomolgus monkeys plasma proteaseLC-MS/MS Cynomolgus monkeys plasmaIn VivoNoneNoneN.A.
5395
310837402019
HSEGTFTSDVSSYLEGQAAKEFIAWLVKGGVKALIDEILAA
SKL-1828741FreeAmidationLinearL3H labeling at Tyr, Ser8 modificationGLP-1 analogsAntidiabetesBlood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous17.4 µ/kg12.9 ± 1.0 (Elimination Half Life)Göttingen minipigs plasma proteaseLC-MS/MS Göttingen minipigs plasmaIn VivoNoneNoneN.A.
5504
306067212019
ACYNEFGCEDFYDIC
BCY-B515AcetylationFreeCyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15)LNoneBicyclic peptide derivativeFor imaging and targeting of proteins overexpressed by tumors37C up to 24 hours4 μmol/L11.5Mouse plasma proteaseLC-MS/MSMouse plasmaIn VitroNoneNoneN.A.
5515
306056342019
pGlu-RPRLSHKGPMPF
(Pyr)1-apelin-1313pGlu = PyroglutamateFreeLinearLNoneApelin analogsHemodynamic Effects In HumansN.A.50 mg/kg11Rats plasma proteaseLC-MS/MSRats plasmaIn VivoNoneNoneN.A.
5517
306056342019
pGlu-RPRLSHKGPMPF
(Pyr)1-apelin-1313pGlu = PyroglutamateFreeLinearLNoneApelin analogsHemodynamic Effects In HumansN.A.10 mg/kg11Dogs plasma proteaseLC-MS/MSDogs plasmaIn VivoNoneNoneN.A.
5538
305040812019
(VPKEG)80
VPKEG80400A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =K, X2= EZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM12.4 ± 0.1N.A.N.A.N.A.In VitroNoneNoneEC50 = 17 nM for GLP1-VPKEG120
5539
305040812019
(VPKEG)120
VPKEG120600A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =K, X2= EZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM12.9 ± 0.2N.A.N.A.N.A.In VitroNoneNoneEC50 = 17 nM for GLP1-VPKEG120
5542
305040812019
(VPKEG)120 
VPKEG120 600A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =K, X2= EZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM12.0 ± 0.4Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneEC50 = 17 nM for GLP1-VPKEG120
5544
305040812019
(VPKDG)120
VPKDG120600A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =K, X2= DZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM10.8 ± 0.2Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneN.A.
5546
305040812019
(VPGAG)120
VPGAG120600A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =G , X2= AZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM10.6 ± 1.6Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneEC50 = 10 nM for GLP1-VPGAG160
5547
305040812019
(VPGAG)160
VPGAG160800A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =G , X2= AZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM12.4 ± 0.8Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneEC50 = 10 nM for GLP1-VPGAG160
5549
305040812019
(VPKDG)120 
VPKDG120 600A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488FreeLinearLX1 =K, X2= DZwitterionic polypeptide derivativeIntrinsically disordered zwitterionic polypeptides for drug delivery10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein300 μM11.8 ± 1 Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneN.A.
5633
305659002018
RGD
DOX@PLEPMPss-cRGD 3PCL-PEGFreeCyclic (N-C terminal end)LNoneSyntheticAnticancerThe plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h)2 mg/kg11.81 ± 0.67 (T1/2b)Mice plasma proteasefluorescence spectrometrymice plasmaIn VivoNoneNoneThe IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1
5634
305659002018
RGD
DOX@Cu-PLEPMPss-cRGD3PCL-PEGFreeCyclic (N-C terminal end)LNoneSyntheticAnticancerThe plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h)2 mg/kg12.20 ± 0.73 (T1/2b)Mice plasma proteasefluorescence spectrometrymice plasmaIn VivoNoneNoneThe IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1
5637
304965752018
GPVPTSKPTTTKGGCHIGRFKSLSPQELASFKKARDALEESLKLKNWSCSSPVFPGNWDLRLLQVRERPVALEAELALTLKVLEAAAGPALEDVLDQPLHTLHHILSQLQACIQPQPTAGPRPRGRLHHWLHRLQEAPKKESAGCLEASVTFNLFRLLTRDLKYVADGNLCLRTSTHPESTSSGSSSSSSSKAPPPSLPSPSRLPGPSDTPILPQNGS
rhIFN-λ1-CTPON218FreeHuman chorionic gonadotropin β subunit carboxyl-terminal peptide (CTP) and an N-glycosylation sequence linked to its C-terminus via linkerLinearLNoneRecombinant human interferon-λ1 derivativeAntiviral, Antiproliferation, And Nk Cell Cytotoxicity-Promoting ActivitiesVenous blood was collected at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h post-injection40 μg/kg10.326 ± 0.87Mice blood proteaseELISAMice blood sampleIn VivoNoneNoneAntiviral activity of the purified rhIFN-λ1 expressed by CHO cells was 2.5 × 105 IU/mg 
5662
300966512018
HGEGTYTNDVTEYLEEEAAKEFIEWLIKGKPSSGAPPPSCHGEGTYTNDVTEYLEEEAAKEFIEWLIKGKPSSGAPPPSC
Analogue 680FreeC terminal Cys extension for bis-maleimide linkageLinearLConjugation of Palmitic acid at Lys20 (single monomer) , dimerizationDimeric lipidated Xenopus GLP-1 analoguesAntidiabetesAt 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball50 nmol/kg10.8 ± 0.8Kunming mice plasma proteaseLC-MS/MSKunming mice plasmaIn VivoNoneNoneEC50 = 1.4 ± 0.5 nM in HEK293 cells
5663
300966512018
HGEGTYTNDVTEYLEEEAAKEFIEWLIKGKPSSGAPPPSCHGEGTYTNDVTEYLEEEAAKEFIEWLIKGKPSSGAPPPSC
Analogue 680FreeC terminal Cys extension for bis-maleimide linkageLinearLConjugation of Palmitic acid at Lys20 (single monomer) , dimerizationDimeric lipidated Xenopus GLP-1 analoguesAntidiabetesBlood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin50 nmol/kg12.9 ± 3.6SD rats plasma proteaseLC-MS/MSSD rats plasmaIn VivoNoneNoneEC50 = 1.4 ± 0.5 nM in HEK293 cells
5693
300127562018
L-threonyl-L-tryptophanyl-L-isoleucyl-L-2,4-diaminobutyryl-L-ornithyl-D-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-tryptophanyl-L-2,4-diaminobutyryl-L-2,4-diaminobutyryl-L-alanyl-L-seryl,D-prolyl-L-prolyl
Murepavadin14FreeFreeCyclic (N-C terminal end)MixAcetateSyntheticAntimicrobialBlood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment2.2 mg/kg14.1Human plasma proteaseLC-MS with electrospray ionization assayHuman plasma (Mild Renal impairment group)In Vivohttps://sci-hub.st/10.1080/14787210.2018.1441024NoneMIC50 = 0.12 mg/L against P. aeruginosa
5700
299264782018
HSQGTFTSDKSEYLDSERARDFVAWLEAG
MEDI038229FreeFreeLinearLPalmitic-Glu conjugation at LysSyntheticAntidiabetes and Non‐Alcoholic SteatohepatitisN.A.30 μg11.43Human plasma proteaseLC-MS Human plasmaIn VivoPubChem CID: 134694273NoneN.A.
5701
299264782018
HSQGTFTSDKSEYLDSERARDFVAWLEAG
MEDI038229FreeFreeLinearLPalmitic-Glu conjugation at LysSyntheticAntidiabetes and Non‐Alcoholic SteatohepatitisN.A.100 μg12.07Human plasma proteaseLC-MS Human plasmaIn VivoPubChem CID: 134694273NoneN.A.
5702
299264782018
HSQGTFTSDKSEYLDSERARDFVAWLEAG
MEDI038229FreeFreeLinearLPalmitic-Glu conjugation at LysSyntheticAntidiabetes and Non‐Alcoholic SteatohepatitisN.A.150 μg10.97Human plasma proteaseLC-MS Human plasmaIn VivoPubChem CID: 134694273NoneN.A.
5705
297992052018
HGEGTYTNDVTEYLEEEAA-X4-EFIEWLIKGKPSSGAPPPS
5b39FreeFreeLinearLX4 = structure given in paperGLP-1 analogsAntidiabetesSerial blood samples (100–200 µL) were collected from fundus venous plexus in microcentrifuge tubes (EDTA containing) at 0, 1, 2, 3, 4, 6, 12, 24 and 48 h50 nmol/kg11.0 ± 1.2SD rats plasma proteaseLC-MS/MS.SD rats plasmaIn VivoNoneNoneN.A.
5742
297321202018
RGDfV
Cilen5FreeFreeMacrocyclic (N-C terminal end)MixMethylation at Phenylalanine (D-form)SyntheticGlioblastoma therapyAt various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h)1 mg/ml12Human serum proteaseHPLCHuman serumIn VitroNoneNoneIC50 value of 11 shows that 11 is poorer than Cilen 
5882
293290722018
YFLNGRPRN
Compound 328AcetylationAmidationLinearLN(benzyl)Gly modfication at position 4NMU-analogsRegulation Of Feeding Behavior, The Stress Response And Nociception37 °C112 µM837.4 ± 27.8Human plasma proteaseRP-HPLCHuman plasma In VitroNoneNoneEC50(nM) = 172.2, IC50(nM) = 83.1 for hNMUR1 and EC50(nM) = 1278, IC50(nM) = 1019 for hNMUR2 
5900
N.A.2018
QRVAAHITGTRGRSNTLSSPNSKNEKALGRKINSWESSRSGHSFLSNLHLRNGELVIHEKGFYYIYSQTYFRFQEEIKENTKNDKQMVQYIYKYTSYPDPILLMKSARNSCWSKDAEYGLYSIYQGGIFELKENDRIFVSVTNEHLIDMDHEASFFGAFLVGSSGSSGSSGSGLPDVASLRQQVEALQGQVQHLQAAFSQYKKVELFPNGQSVGEKIFKTAGFVKPFTEAQLLCTQAGGQLASPRSAAENAALQQLVVAKNEAAFLSMTDSKTEGKFTYPTGESLVYSNWAPGEPNDDGGSEDCVEIDTNGKWNDRACGEKRLVVCEFGGSPSSSSSSAWSHPQFEK
TRAIL-ASPD_F335D 347FreeC-type lectin domain of human SP-D joined with Strep-tag II using linkerLinearLPhe355 -> Asp355 modificationTrail-SPD Fusion ProteinTherapeutic, diagnostic and/or research applicationsSerum samples were collected after several time points (predose, 5 min., 30 min., 2H, 6H and 24H)10 μg 14CD1 mice serum proteaseELISACD1 mice serumIn VivoNoneEP 17197297 AFive hours of co-incubation of primary human hepatocytes with trimeric TRAIL-ASPD_F335D together with chemotherapeutic drugs induced no caspase activity (E)
5954
288214622017
MTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIQKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNESGSSGGSGSSGGSGGGDEADGSRGSQKAGVDE
LCFN144183FreeFusing the XTEN peptide of 144 amino acids through a linkerLinearLGly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocageswtFN derivativeAntitumorN.A.50 mg/kg11.3 ± 1.0Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneN.A.
5955
288214622017
MTTASTSQVRQNYHQDSEAAINRQINLELYASYVYLSMSYYFDRDDVALKNFAKYFLHQSHEEREHAEKLMKLQNQRGGRIFLQDIQKPDCDDWESGLNAMECALHLEKNVNQSLLELHKLATDKNDPHLCDFIETHYLNEQVKAIKELGDHVTNLRKMGAPESGLAEYLFDKHTLGDSDNESGSSGGSGSSGGSGGGDEADGSRGSQKAGVDE
LCFN288183FreeFusing the XTEN peptide of 288 amino acids through a linkerLinearLGly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocageswtFN derivativeAntitumorN.A.50 mg/kg10.2 ± 0.3Mice plasma proteaseFluorescence assayMice plasmaIn VivoNoneNoneN.A.
5978
287144752017
EYEKEYE
Tag7Fluorescein (F) AmidationLinearLLys4 linked with Palm fatty acidSyntheticIncreases Half LifeN.A.0.25 mg/kg12.3 ± 0.4 (T1/2b)Rats plasma proteaseRP-HPLC using a fluorescence detectorRats plasmaIn VivoNoneNoneAlbumin binding (Kd) (nM) = 220±30 for rat albumin
6029
283567332017
MHSDAVFTDQYTRLRKQLAAKKYLQSLKQKRY
SCD32FreeChitosan-modified SeNP (SC)LinearLNonePeptide-conjugated selenium nanoparticlesAntidiabetesOrbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing1 mg/kg14.12DB/DB mice orbital blood proteaseLC-MS/MSDB/DB mice orbital blood sampleIn VivoNoneNoneIC50 of SC for INS-1 cells was 66.10 μM
6035
282818682017
DAHKSEVAHRFKDLGEENFKALVLIAFAQYLQQCPFEDHVKLVNEVTEFAKTCVADESAENCDKSLHTLFGDKLCTVATLRETYGEMADCCAKQEPERNECFLQHKDDNPNLPRLVRPEVDVMCTAFHDNEETFLKKYLYEIARRHPYFYAPELLFFAKRYKAAFTECCQAADKAACLLPKLDELRDEGKASSAKQRLKCASLQKFGERAFKAWAVARLSQRFPKAEFAEVSKLVTDLTKVHTECCHGDLLECADDRADLAKYICENQDSISSKLKECCEKPLLEKSHCIAEVENDEMPADLPSLAADFVESKDVCKNYAEAKDVFLGMFLYEYARRHPDYSVVLLLRLAKTYETTLEKCCAAADPHECYAKVFDEFKPLVEEPQNLIKQNCELFEQLGEYKFQNALLVRYTKKVPQVSTPTLVEVSRNLGKVGSKCCKHPEAKRMPCAEDYLSVVLNQLCVLHEKTPVSDRVTKCCTESLVNRRPCFSALEVDETYVPKEFNAETFTFHADICTLSEKERQIKKQTALVELVKHKPKATKEQLKAVMDDFAAFVEKCCKADDKETCFAEEGKKLVAASQAALGLMALCKFCDVRFSTCDNQKSCMSNCSITSICEKPQEVCVAVWRKNDENITLETVCHDPKLPYHDFILEDAASPTCIMKEKKKPGETFFMCSCSSDECNDNIIFSEEYNTSNPD
HSA-eTGFBR2697FreeeTGFBR2 fused at the C-terminal of HSALinearLNoneSyntheticNeutralize TGF-Β1 activityBlood samples were collected 5 min, 15 min, 30 min, 1 h, 2 h, 6 h,12 h, 24 h3 nmol/kg11.84Mice serum proteaseHuman TGF-b RII Duo Set ELISA Mice serumIn Vivopdb id: 4P7U, 7DJNNoneKD = 1.42* 10-8M of HSA-eTGFBR2 for TGF-B1
6144
270584302016
KIKIPWGKVKDFLVGGMKAV
Bicarinalin20FreeAmidationLinearLNoneAnt venom peptideAntimicrobial37 ◦C until 48 hN.A.15Human serum proteaseLC-MSHuman serumIn VitroNoneNoneBicarinalin displayed no cytotoxicity against human lymphocytes in concentrations ranging from 0.066 to 8.5 mol L−1 and its LC50 value was 67.8 mol L−1
6145
270584302016
KIKIPWGKVKDFLVGGMKAV
Bicarinalin20FreeAmidationLinearLNoneAnt venom peptideAntimicrobial37 ◦C until 48 hN.A.15Human serum proteaseLC-MSHuman serumIn VitroNoneNoneMIC [micromole/L] = 24.4, 5.8, 12.2, 8.7, 5.4 for E.coli, C.sakazakii, P.aeruginosa CIP 82118, P.aeruginosa [R]ATCC 15442, S.enterica respectively. 
6146
270584302016
KIKIPWGKVKDFLVGGMKAV
Bicarinalin20FreeAmidationLinearLNoneAnt venom peptideAntimicrobial37 ◦C until 48 hN.A.15Human serum proteaseLC-MSHuman serumIn VitroNoneNoneMIC [micromole/L] = 12.2, 3, 8.7, 0.45, 24.4 for E.hirae, S.aureus, MRSA, S.xylosus, B.subtilis respectively
6147
270584302016
KIKIPWGKVKDFLVGGMKAV
Bicarinalin20FreeAmidationLinearLNoneAnt venom peptideAntimicrobial37 ◦C until 48 hN.A.15Human serum proteaseLC-MSHuman serumIn VitroNoneNoneMIC [micromole/L] = 0.75, 17.3, 17.3, 97.5, 6.1 for A.niger, C.albicans, C.albicans[R], G.candidum, S.cerevisiae and MIC[micromole/L] = 1.5 for L.infantum
6148
322632292016
RGDfC
iT-P/PTX NPs5FreeTPGS(D-a-tocopherol polyethylene glycol succinate) linked with poly(lactide) using disulfide linkage, cRGD further conjugated to NP surfaceCyclic (RGDfC)MixD-Phe at position 4SyntheticAnticancerBlood samples were collected in EP tubes containing 20 mL of 1000 U heparin per mL at 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h for each group.10 mg/ kg12.68 ± 0.81 SD rats plasma proteaseHPLCSD rats plasmaIn VivoNoneNoneIC50 = 1.90 ± 0.28 mg/mL incubated with A2780 cell 
6165
268083052016
SCNTATCVTHRLAGLLSRSGGVVKDNFVPTNVGSEAF
αAnalogue37Fatty acid moiety attached to Ser1 at N terminalAmidationCyclic (Disulfide Bridge Between Positions 2 And 7)LNoneCGRP analogueVasodilatory effectBlood (200 µl) was sampled from vena sublingualis from anaesthetised rats at pre-dose and at 0.5, 1, 3, 7 and 24 h post dosing151 nmol/kg10.2 ± 0.9 SD rats plasma proteaseELISASD rats plasmaIn Vivohttps://sci-hub.st/10.1126/science.2994212, NoneN.A.
6169
268081992016
LRHYLNLLTRQRY
PYY24–36-Leu31 conjugates 513R5( structure given in paper) at NH terminalAmidationLinearLLeu31 substituitionsPYY 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>12SD rats plasma proteaseLC–MS/MSSD rats plasmaIn VitroNoneNoneHSA binding correlated well with plasma stability
6170
268081992016
LRHYLNLLTRQRY
PYY24–36-Leu31 conjugates 713R7( structure given in paper) at NH terminalAmidationLinearLLeu31 substituitionsPYY 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>12SD rats plasma proteaseLC–MS/MSSD rats plasmaIn VitroNoneNoneHSA binding correlated well with plasma stability
6171
268081992016
LRHYLNLLTRQRY
PYY24–36-Leu31 conjugates 913R9( structure given in paper) at NH terminalAmidationLinearLLeu31 substituitionsPYY 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>12SD rats plasma proteaseLC–MS/MSSD rats plasmaIn VitroNoneNoneHSA binding correlated well with plasma stability
6175
268064902016
SSSSKAPPPSLPSPSRLPGPSDTPILPQCDLPQTHSLGSRRTLMLLAQMRRISLFSCLKDRHDFGFPQEEFGNQFQKAETIPVLHEMIQQIFNLFSTKDSSAAWDETLLDKFYTELYQQLNDLEACVIQGVGVTETPLMNEDSILAVRKYFQRITLYLKEKKYSPCAWEVVRAEIMRSFSLSTNLQESLRSKE-SSSSKAPPPSLPSPSRLPGPSDTPILPQ
CTP-IFN-CTP221CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG))CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG))LinearLNoneRecombinant human IFN-α2bAntiviral, AnticancerN.A.1*106 U / 200 g13.4 ± 1.5 (Elimination Half Life)Wistar rats plasma proteaseN.A.Female Wistar rats plasmaIn VivoNoneNoneSpecific antiviral bioactivity (U ng−1) = 44 ± 3, Specific antiproliferative bioactivity (U ng−1) = 9 ± 1
6189
267254262016
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicN.A.23.88 nmol/mL10.16Carboxy-Peptidase A Mass spectrometryIntestinal fluid buffer (pH 6.8) with CPA (0.2 U/mL)In VitroPDB id: 7MLLNoneN.A.
6190
267254262016
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicN.A.23.88 nmol/mL12.38TrypsinMass spectrometryIntestinal fluid buffer (pH 6.8) with Trypsin (0.2 U/mL)In VitroPDB id: 7MLLNoneN.A.
6191
267254262016
HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS
Exenatide39FreeAmidationLinearLNoneExendin-4 analogsAntihyperglycemicN.A.23.88 nmol/mL14.28PepsinMass spectrometryGastric fluid solution (pH 1.2) with Pepsin (0.2 U/mL)In VitroPDB id: 7MLLNoneN.A.
6211
267138392016
SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ
MOD-4023275CTP fused to hGH2 CTP fusedLinearLNoneSyntheticTreatment of GHDDay 11.5 mg/kg12.76 ± 2.06Monkeys serum proteaseSandwich ELISAMonkeys serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGUNoneEC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)
6218
267138392016
SSSSKAPPPSLPSPSRLPGPSDTPILPQFPTIPLSRLFQNAMLRAHRLHQLAFDTYEEFEEAYIPKEQKYSFLQAPQASLCFSESIPTPSNREQAQQKSNLQLLRISLLLIQSWLEPVGFLRSVFANSLVYGASDSDVYDLLKDLEEGIQTLMGRLEDGSPRTGQAFKQTYAKFDANSHNDDALLKNYGLLYCFRKDMDKVETFLRIVQCRSVEGSCGF-(SSSSKAPPPSLPSPSRLPGPSDTPILPQSSSSKAPPPSLPSPSRLPGPSDTPILPQ
MOD-4023275CTP fused to hGH2 CTP fusedLinearLNoneSyntheticTreatment of GHDDay 1811.5 mg/kg17.01 ± 6.91Monkeys serum proteaseSandwich ELISAMonkeys serumIn Vivohttps://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGUNoneEC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells)