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Browsing Year-wise: 1996 - 2000

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IDPMIDYEARSequenceNameLengthN-ter MODC-ter MODLinear/CyclicChiralityChem-MODOriginNatureIncubation TimeConcentrationHalf LifeUnits Half LifeProteaseAssayTest SampleVivo/VitroReferencePatent No.Activity
1049
104954241999
AAGIGILTV
MART-127 €“359FreeFreeLinearLNoneSyntheticImmunogenic peptidesNot given1 µM22Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneIC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 0.5 µM
1050
104954241999
AAGIGILTV
PEG-MART-19FreePegylationLinearLNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneIC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is >35 µM
1051
104954241999
aAGIGILTv
D-MART-19FreeFreeLinearMixNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneNot tested
1052
104954241999
AAGIGILTV
Glyco-MART-19Asn(β-D-GlcNHAc)FreeLinearLNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneNot tested
1053
104954241999
AAGIGILTV
Cap-MART-19AcetylationAmidationLinearLNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneIC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 65 µM
1054
104954241999
AAGIGILTV
N-MART-19AcetylationFreeLinearLNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneIC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 35 µM
1055
104954241999
AAGIGILTV
C-MART-19FreeAmidationLinearLNoneSyntheticImmunogenic peptidesNot givenNot givenStability increasedHuman plasma proteases and proteases of VMM5 cytotoxic T-lymphocyteNot mentionedVMM5 cytotoxic T-lymphocyte line incubated in human plasmain vitroNoneNoneIC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 7 µM
1082
110994872000
RQIKIWFQNRRMKWKKNELKRAFAALRDQI
Int-H1-S6A,F8A30FreeFreeLinearLNoneC-Myc derivativeAntiproliferative and proapoptoticNot reportedNot mentioned11.95Fetal calf serum proteasesHPLCFetal bovine serum batch1in vitroNoneNoneNot reported
1083
110994872000
RQIKIWFQNRRMKWKKNELKRAFAALRDQI
Int-H1-S6A,F8A30FreeFreeLinearLNoneC-Myc derivativeAntiproliferative and proapoptoticNot reportedNot mentioned18.73Fetal calf serum proteasesHPLCFetal bovine serum batch2in vitroNoneNoneNot reported
1084
110994872000
RQIKIWFQNRRMKWKKNELKRAFAALRDQI
Int-H1-S6A,F8A30FreeFreeLinearLNoneC-Myc derivativeAntiproliferative and proapoptoticNot reportedNot mentioned4.62Fetal calf serum proteasesHPLCFetal bovine serum batch3in vitroNoneNoneNot reported
1085
110994872000
RQIKIWFQNRRMKWKKNELKRAFAALRDQI
Int-H1-S6A,F8A30FreeFreeLinearLNoneC-Myc derivativeAntiproliferative and proapoptoticNot reportedNot mentioned7.29Fetal calf serum proteasesHPLCFetal bovine serum batch4in vitroNoneNoneNot reported
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
1116
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=3 µg/ml for M. Luteus ATCC 9341
1117
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for M. Luteus ATCC 9342
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
1119
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=3.12 µg/ml for M. Luteus ATCC 9344
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
1124
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=10 µg/ml for S. Aureus ATCC 6540
1125
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 µg/ml for S. Aureus ATCC 6541
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
1127
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=9 µg/ml for S. Aureus ATCC 6543
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
1132
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=1.56 µg/ml for S. Epidemidis ATCC 12229
1133
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse 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
1135
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=2 µg/ml for S. Epidemidis ATCC 12228
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
1140
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=50 µg/ml for MRSA SR 1553
1141
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=>100 µg/ml for MRSA SR 1554
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
1143
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=38 µg/ml for MRSA SR 1556
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
1148
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 µg/ml for M. smegmatis ATCC 607
1149
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 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
1151
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for M. smegmatis ATCC 613
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
1156
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=12.5 µg/ml for E. coli ATCC 2592
1157
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=31 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
1159
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=19 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
1164
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=6.25 µg/ml for P. aeruginosa ATCC 9027
1165
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=25 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
1167
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=6.25 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
1172
104617471998
KKΨ[CH2NH]VVFKVKFk
KSL310FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=6.25 µg/ml for C. albicans ATCC 36232
1173
104617471998
KΨ[CH2NH]KΨ[CH2NH]VVFKVKFk
KSL410FreeFreeLinearMixReduced amide bonds Ψ(CH2NH)SyntheticAntimicrobialNot reported100 µg/mL>81Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=31 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
1175
104617471998
KΨ[CH2OCONH]KΨ[CH2OCONH]VVFKVKFk
KSL610FreeFreeLinearMixReduced carbamate Ψ(CH2OCONH)SyntheticAntimicrobialNot reported100 µg/mL67Mouse serum proteasesRP-HPLCMouse serumin vitroNoneNoneMIC=11 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
1183
105412991999
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR
Epoetin166FreeFreeCyclicLThree N-linked carbohydrate chainsRecombinant human erythropoietinStimulates erythropoiesisNot mentionedNot mentioned8.5 ±2.4Human blood proteasesELISASubcutaneously injected into patients with end-stage renal failurein vivohttp://www.drugbank.ca/drugs/DB00016NoneNot reported
1184
105412991999
APPRLICDSRVLERYLLEAKEAENITTGCAEHCSLNENITVPDTKVNFYAWKRMEVGQQAVEVWQGLALLSEAVLRGQALLVNSSQPWEPLQLHVDKAVSGLRSLTTLLRALGAQKEAISPPDAASAAPLRTITADTFRKLFRVYSNFLRGKLKLYTGEACRTGDR
Novel erythropoiesis stimulating protein (NESP)166FreeFreeCyclicLFive N-linked carbohydrate chainsHyperglycosylated analogue of recombinant human erythropoietinStimulates erythropoiesisNot mentionedNot mentioned25.3 ±2.2Human blood proteasesELISASubcutaneously injected into patients with end-stage renal failurein vivohttp://www.drugbank.ca/drugs/DB00017NoneNot reported
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
1670
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 minNot mentioned10 ±1Angiotensin-converting enzymeRadioimmunoassay and HPLCBlood sample of normotensive Sprague-Dawley ratin vivoNoneNoneNot mentioned
1671
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg10 ±1Angiotensin-converting enzymeRadioimmunoassay and HPLCBlood sample of anesthetized spontaneously hypertensive ratin vivoNoneNoneNot mentioned
1672
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg9 ±1Angiotensin-converting enzymeRadioimmunoassay and HPLCBlood sample of mRen-2 transgenic ratin vivoNoneNoneNot mentioned
1673
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~11 ±1Angiotensin-converting enzyme and losartan(AT1 antagonist)Radioimmunoassay and HPLCBlood sample of normotensive Sprague-Dawley ratin vivoNoneNoneNot mentioned
1674
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~11 ±1Angiotensin-converting enzyme and losartan(AT1 antagonist)Radioimmunoassay and HPLCBlood sample of anesthetized spontaneously hypertensive ratin vivoNoneNoneNot mentioned
1675
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~14 ±1Angiotensin-converting enzyme and losartan(AT1 antagonist)Radioimmunoassay and HPLCBlood sample of mRen-2 transgenic ratin vivoNoneNoneNot mentioned
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
1677
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~44 ±1Angiotensin-converting enzyme and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of anesthetized spontaneously hypertensive ratin vivoNoneNoneNot mentioned
1678
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~29 ±1Angiotensin-converting enzyme and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of mRen-2 transgenic ratin vivoNoneNoneNot mentioned
1679
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~45 ±1Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of normotensive Sprague-Dawley ratin vivoNoneNoneNot mentioned
1680
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~49 ±1Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of anesthetized spontaneously hypertensive ratin vivoNoneNoneNot mentioned
1681
97406161998
DRVYIHP
Ang-(1-7)7FreeFreeLinearLNoneAngiotensinogenAntihypertensive30 min10 µg~40 ±1Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor)Radioimmunoassay and HPLCBlood sample of mRen-2 transgenic 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
1685
98226651998
MLPGLALLLLAAWTARALEVPYPYDVPDYASNKGAIIGLMVGGVVIATVIVITLVVMLKKKQYEQKLISEEDL
H26-57C74FreeFreeLinearLNoneAmyloid precursor proteinNot mentioned40 minutesNot mentioned10γ-secretase (protease) ALLN(protease inhibitor)Pulse chase experimentHuman embryonic kidney cellsin vitroNoneNoneNot mentioned
1702
106111391999
H(2me)wAWfK
Hexarelin6FreeAmidationLinearMix2me-2-methyl(tryptophan)Analog of GHRP-6Peptidyl growth hormone causing GH releasing effect.Not reported10 to 25 iu of oxytocin75.9 ±9.3Blood proteasesLC-MS/MSIntravenous injection,Blood sample from male Sprague-Dawley ratsin vivoNoneNoneNot mentioned
1703
106111391999
H(2me)wAWfK
Hexarelin6FreeAmidationLinearMix2me-2-methyl(tryptophan)Analog of GHRP-6Peptidyl growth hormone causing GH releasing effect.Not reported5 µg/kg71.9 ±11.2Blood proteasesLC-MS/MSIntravenous injection,Blood sample from male Sprague-Dawley ratsin vivoNoneNoneNot mentioned
1704
106111391999
H(2me)wAWfK
Hexarelin6FreeAmidationLinearMix2me-2-methyl(tryptophan)Analog of GHRP-6Peptidyl growth hormone causing GH releasing effect.Not reported10 µg/kg61.4 ±9.5Blood proteasesLC-MS/MSIntravenous injection,Blood sample from male Sprague-Dawley ratsin vivoNoneNoneNot 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.
1707
108713212000
RPPGF
BK1-55FreeFreeLinearLNoneMetabolite of bradykininNot mentionedNot reported106 cpm/200μl/mouse~90Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidaseHPLC-ESI-MSIntravenous injection of Bradykinin,Human blood samplein vivoNoneNoneNot mentioned
1708
108713212000
RPPGFSPFR
Bradykinin9FreeFreeLinearLNoneHuman blood plasmaCardioprotective effectsNot reported106 cpm/200μl/mouseNot measured as peptide degraded rapidly<30 approx.Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidaseHPLC-ESI-MSHuman blood samplein vivoNoneNoneNot 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%
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
2078
89104261996
GCTFRRLKWKCG
LALF-10 (38 €“45)12FreeFreeCyclic (C2-C11)LNoneAnalogue of Limulus anti-lipopolysaccharide factorAntibacterialNot reported2.5 µg/ml77Proteases present in fetal calf serumRP-HPLCFetal calf serumin vitroNoneNoneLD50=2.58 mg/ml
2079
89104261996
GCKPTFRRLKWKYKCG
LALF-14 (36 €“47)16FreeFreeCyclic (C2-C15)LNoneAnalogue of Limulus anti-lipopolysaccharide factorAntibacterialNot reported2.5 µg/ml84Proteases present in fetal calf serumRP-HPLCFetal calf serumin vitroNoneNoneLD50=2.33 mg/ml
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
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
2337
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/kg64 (t1/2 β)Dog blood plasma proteasesHPLC-MSIntravenous administered to Dogin vivoNoneNoneNot tested
2338
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min0.10mg/kg64 (t1/2 β)Rabbit blood plasma proteasesHPLC-MSIntravenous administered to Rabbitin vivoNoneNoneNot tested
2339
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min0.10mg/kg68 (t1/2 β)Monkey blood plasma proteasesHPLC-MSIntravenous administered to Monkeyin vivoNoneNoneNot tested
2340
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min5 mg/kg73 (t1/2 β)Rat blood plasma proteasesHPLC-MSOrally 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
2343
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min50 mg/kg80Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2344
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min300 mg/kg99Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2345
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min500 mg/kg122Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2346
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min1000 mg/kg204Rat 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
2348
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day5 mg/kg74Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2349
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day50 mg/kg80Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2350
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day50 mg/kg71Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2351
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day300 mg/kg99Rat blood plasma proteasesHPLC-MSOrally administered to Ratin vivoNoneNoneNot tested
2352
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day300 mg/kg100Rat 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
2357
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant1 day300 mg/kg75Dog blood plasma proteasesHPLC-MSOrally administered to Dogin vivoNoneNoneNot tested
2358
89914891996
RPD
IRI-695 peptide3AcetylationIsobutyl citrateLinearLC14 RadiolabelingSyntheticAnxiolytic and antidepressant28 day300 mg/kg76Dog 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.
2362
90626851997
NSPR
Analogue of [Cys6]AVP(5-8)4FreeFreeLinearLNoneHuman kidney cellsAntidiuretic hormone5, 10, 30, 60 and 120 min10 ng/kg223Rat 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
2364
94214011998
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial Natriuretic peptide28FreeFreeLinearLNoneHuman Heart muscle cellsAntihypertensive0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min2 μg0.8 ±0.1 (t1/2 fast 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.
2365
94214011998
SLRRSSCFGGRMDRIGAQSGLGCNSFRY
Atrial Natriuretic peptide28FreeFreeLinearLNoneHuman Heart muscle cellsAntihypertensive0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min2 μg0.9 ±0.1 (t1/2 fast 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.
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.
2368
95898221998
Mpr-Har-GDWPC
Eptifibatide7Mpr=mercaptopropionylAmidationCyclic (disulfide bridge between cysteine and mercaptopropionyl)LNoneVenom of pygmy rattlesnakeAntithrombotic1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours135 μg/kg1.13 ±0.17 (t1/2 termination)Human blood plasma proteasesHPLCIntravenous injection to Humanin vitrohttp://www.prospecbio.com/Eptifibatide_11_124/NoneNot tested
2369
95898221998
Mpr-Har-GDWPC
Eptifibatide7Mpr=mercaptopropionylAmidationCyclic (disulfide bridge between cysteine amide and mercaptopropionyl)LNoneVenom of pygmy rattlesnakeAntithrombotic1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours135 μg/kg5 ±2.5 (t1/2 distribution)Human blood plasma proteasesHPLCIntravenous injection to Humanin vitrohttp://www.prospecbio.com/Eptifibatide_11_124/NoneNot tested
2370
99321631998
VVVPP
Cemadotin-HCl5FreeFreeLinearLNoneSynthetic analogue of Dolastatin 15Antimitotic24 hour10 - 27.5mg10Human blood proteasesRadioimmunoassayIntravenous administration to humanin vivoNoneNoneCancer patient was administered with Cemadotin for 24 hours intravenously at dose of 10mg. Reduction in liver metastasis was observed by sonographic examination.
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
2373
103544131999
YGG
Thioimreg compound 83FreeFreeLinearLPeptide bonds at position 2,3 was replaced by thioamide linkageThioanalogue of natural ImregImmunostimulant3.5 hoursNot given>180Rat blood proteasesHPLCRat whole bloodin vitroNoneNoneA weak in vitro induction of T (PHA) and B (PWM) cell proliferation (1.5 to 2-fold increase) by the thioanalogues
2374
105732951999
DPLPEF
Enkephalin6FreeAmidationLinearLNoneNatural (Human brain)Analgesic0, 60, 120, 180, and 300 min1mM30Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2375
105732951999
DPLPEF
Enkephalin analog6FreeFreeLinearLNoneDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2376
105732951999
p-[Cl-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara chlorination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2377
105732951999
p-[Br-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara bromination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2378
105732951999
p-[F-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara florination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2379
105732951999
p-[I-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara iodination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse plasma proteasesHPLC , reverse phase HPLC, Partition coefficientMouse plasmain vitroNoneNoneNot tested
2380
105732951999
DPLPEF
Enkephalin6FreeAmidationLinearLNoneNatural (Human brain)Analgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin vitroNoneNoneNot tested
2381
105732951999
DPLPEF
Enkephalin analog6FreeFreeLinearLHydroxylation of amino group of PhenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin vitroNoneNoneNot tested
2382
105732951999
p-[Cl-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara chlorination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin vitroNoneNoneNot tested
2383
105732951999
p-[Br-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara bromination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin vitroNoneNoneNot tested
2384
105732951999
p-[F-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara florination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin vitroNoneNoneNot tested
2385
105732951999
p-[I-Phe4]DPLPEF
Enkephalin analog6FreeFreeLinearLPara iodination of amino group of phenylalanineDerivative of Natural enkephalinAnalgesic0, 60, 120, 180, and 300 min1mM>300Mouse brain proteasesHPLC , reverse phase HPLC, Partition coefficientMouse brain proteasesin 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
2387
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 nM0.62 ±0.05 (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.
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
2415
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/kg106 ±22 (t1/2 β)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
2417
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/kg112 ±41 (t1/2 β)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
2419
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/kg103 ±19 (t1/2 β)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
2421
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/kg173 ±13 (t1/2 β)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
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.
2537
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 μl203 ±10.2 (t1/2β)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.
2538
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 μl185.4 ±4.7 (t1/2β)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.
2539
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 μl111.1 ±3.9 (t1/2β)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.
2540
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 μl140.2 ±2.5 (t1/2β)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.
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
3050
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEGAmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg21.6Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Male ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,262×103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05×106/mm3 to 5.56×106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds.
3051
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg30.2Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Female ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,262×103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05×106/mm3 to 5.56×106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds.
3052
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg23Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Male ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,243×103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds.
3053
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg20.4Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Female ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,243×103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds.
3054
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg18.2Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Male ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,304×103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05×106/mm3 to 5.52×106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds.
3055
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg19.4Rats blood proteasesRadioimmunoassayIntravenous injection of the peptide in Hans Wistar Female ratin vivoNoneNonePlatelet count increased from 1,504×103/mm3 to 2,304×103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05×106/mm3 to 5.52×106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds.
3056
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported10μg/kg37Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3057
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported2μg/kg68Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3058
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported10μg/kg47Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3059
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported25μg/kg45Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3060
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported100μg/kg45Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3061
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported2μg/kg39Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3062
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopeniaNot reported10μg/kg45Monkey blood proteasesRadioimmunoassaySubcutaneous injection in cynomolgus monkeysin vivoNoneNoneNot mentioned
3063
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg following dose 126.1Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3064
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg following dose 125.4Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3065
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg following dose 123.4Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3066
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg following dose 123.7Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3067
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg following dose 133.8Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3068
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg following dose 124.2Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3069
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg following dose 1427.2Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3070
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours500μg/kg following dose 1432.7Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds.
3071
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg following dose 1444Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3072
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours1000μg/kg following dose 1425.1Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds.
3073
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg following dose 1439.3Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus male monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.
3074
106061601999
(IEGPTLRQ-Npa-LAAR-Sar)2K
GW39505829Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O]AmidationLinear (branched)LNpa-napthylalanine,Sar-sarcosineAF15705(substituted thrombopoietin mimetic peptide)Treatment of thrombocytopenia48 hours2000μg/kg following dose 1431.3Monkey blood proteasesRadioimmunoassayIntravenous injection in cynomolgus female monkeyin vivoNoneNonePlatelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds.