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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 15012592 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | >12 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-pyroglutamyl-GLP-1 | 30 | PyroGlutamic acid at 1st position | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | >12 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | >12 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-pyroglutamyl-GLP-1 | 30 | PyroGlutamic acid at 1st position | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | >12 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 11.95 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch1 | in vitro | None | None | Not reported | |||
| 15246869 | 2004 | (Abu8)GLP-1 | 30 | Free | Free | Linear | L | 2-aminobutyric acid (Abu) | Synthetic | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=4.7 ±1.3nM | |||
| 15246869 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon-like peptide-1(7-36)amide | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma proteases except DPP | Radioimmunoassay | Human plasma+DPA (DPA is DPP inhibitor) | in vitro | None | None | cAMP EC50=6.1 ±1.8nM | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma proteases except DPP | Radioimmunoassay | Human plasma+DPA (DPA is DPP inhibitor) | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 14759771 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Amidation | Linear | L | None | Derivative of glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | >12 | Purified DPP IV | ESI-MS | Purified DPP IV | in vitro | None | None | 12 ±0.4% insulin intensity in ARIP cells | |||
| 14759771 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Amidation | Linear | L | None | Derivative of glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | >12 | Serum proteases | ESI-MS | Serum | in vitro | None | None | 16 ±0.1% glucokinase intensity in ARIP cells | |||
| 21114599 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 10.3 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.08 ±0.03nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib8]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 12.1 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.29 ±0.22nM for cAMP stimulation | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.019 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.043 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.079 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.038 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.196 µg/ml against 098-T651 virus | |||
| 15587934 | 2004 | AlbuBNP | 32 | Human serum albumin | Free | Linear | L | None | B-type cardiac natriuretic peptides fused to HAS at N-terminal | Vasodilator | Not reported | 2.19 mg/kg | 11.2 | Mouse blood proteases | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =28.4 ± 1.2 nM | |||
| 19533722 | 2009 | C6 | 12 | Free | Free | Linear | L | None | Synthetic peptide | Mimic putative inhibitor epitopes (mimotopes), | Not reported | 150 µM | ~12 | Human plasma proteases | ELISA | Human plasma | in vitro | None | None | IC50 =30 €“50 µM | |||
| N.A. | 2004 | [NMeEI, amide]-Melan-A | 10 | Free | Amidation | Linear | L | Methylation of nitrogen of amide bond b/w Glu1 and Leu2 (NMe) | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 1 nM | |||
| N.A. | 2004 | [pEI, amide]-Melan-A | 10 | PyroGlutamic acid at 1st position | Amidation | Linear | L | Pyroglutamic acid | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 11 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.3 nM | |||
| N.A. | 2004 | [βAl, amide] -Melan-A | 10 | Beta-Alanine1 | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 11 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.03 nM | |||
| N.A. | 2004 | [βDl, amide] -Melan-A | 10 | Beta-Asp1 | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 10 nM | |||
| N.A. | 2004 | [NOHG1, amide]-Melan-A | 10 | Hydroxylation of N-terminal of Glycine | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 13 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.04 nM | |||
| N.A. | 2004 | [αMeL2, V10-amide]-Melan-A | 10 | Free | Amidation | Linear | L | Methylation of carboxyl of Leu2 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(2.5 nM); isomer2(0.1 nM) | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 11.8 | SCLC proteases | RP-HPLC and Electrochemical Detection | Small cell lung cancer (SCLC) | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 14.6 | Mouse liver proteases | RP-HPLC and Electrochemical Detection | Mouse liver homogenate | in vitro | None | None | Act as growth factors | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 1.25 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 32 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 2.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 34 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 5.0 μg/kg | 15 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 35 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 10 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 36 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 12.5 μg/kg | 12 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 37 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 15 μg/kg | 13 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 38 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 17.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 39 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 20 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 19805567 | 2010 | Enfuvirtide-PEG12-CP | 37 | Acetylation | Free | Linear | L | Mal-PEG12-CP was conjugated to Cys-enfuvirtide | Enfuvirtide conjugate | Antiretroviral fusion inhibitor | 5, 15, and 30 min and 1, 2, 4, 8, 24, and 48 h after drug injection | dose, 4 mg/kg of body weight | 10.4 | Wistar rats blood protease | LC-MS/MS | Female Wistar rats | in vivo | None | None | The enfuvirtide-CP conjugates displayed similar EC50s that ranged from 51 nM to 72 nM | |||
| 17682073 | 2007 | NC100668 | 13 | Acetylation | Tc chelator (NC100194) | Linear | L | Tyr residue at 8 position is Iodionated | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Tracer tested for nuclear medical imaging | 1, 1.5, 3, 6, 12, and 24 hours | 20, 100, 500, 1000, and 2000 μg | 10.5 (terminal elimination) | Human plasma proteases | LC-MS | Injected in human plasma | in vivo | None | None | Not reported | |||
| 8218482 | 1993 | RGD containing peptide | 5 | Free | Free | Linear | L | I125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymer | Extra Cellular Matrix proteins | Antitumor peptide | Not mentioned | 0.2 mL | 11.3 (t1/2 second phase) | Mice blood proteases | Radioimmunoassay | Intravenously injected to C57BL6 mice | in vivo | None | None | Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface. | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.02 mg/kg | 14.6 ±4.3 | Monkey plasma proteases | Competitive ELISA | Monkey plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 6 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 15 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 18.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 8 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 12.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 7.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 10 | 30 | Free | Amidation | Linear | L | X-1 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 11.8 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =12.1 ± 0.5 pM in HEK-293 cells | |||
| 25039358 | 2014 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 14 .9 ±0.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells | |||
| 25894376 | 2015 | P32 (Fibroblast growth factor 2- binding peptide derivative) | 11 | Free | Amidation | Linear | Mix | None | Fibroblast growth factor 2- binding peptide derivative | Anti-proliferative | 37 °C for 1-48hours | 0.3478μM | 12 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | P32 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 | |||
| 25771000 | 2015 | MHDBAY (Recombinant PACAP-derived peptide) | 45 | Free | Free | Linear | L | None | Synthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide) | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | 12.19 | db/db mice plasma proteases | LC-MS/MS | (Dose i/v injected)Mice plasma | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control | |||
| 25771000 | 2015 | MHDBAY (Recombinant PACAP-derived peptide) | 45 | Free | Free | Linear | L | None | Synthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide) | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | >12 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 10.8 ±0.8 | Pig blood proteases | Radioimmunoassay and HPLC | Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 11.9 ±0.7 | Pig plasma proteases | Radioimmunoassay and HPLC | Female pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 13 ±0.7 | Human plasma proteases + DPP IV | MS | Human Plasma+ Heparin | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | Apr-24 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 12 ±3 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 04 to 18 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 12 ±1.0 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | GIP (1-42) (Glucosedependent insulinotropic polypeptide) | 42 | Free | Free | Linear | L | None | Proprotein of gastrointestinal tract | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | May-20 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | GIP (1-42) (Glucosedependent insulinotropic polypeptide) | 42 | Free | Free | Linear | L | None | Proprotein of gastrointestinal tract | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | May-20 | Human serum proteases + DPP IV | MS | Serum | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | Glucagon | 29 | Free | Free | Linear | L | None | Peptide hormone of pancrease | Regulates hypoglycemia | Room Temp | 0.4 µM | May-20 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26308095 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | Acylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Upregulates intracellular cAMP resulting in the release of insulin | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 14.4 hours | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26337231 | 2015 | RMP-16 (Recombinant slow-release TNF α-derived peptide) | 32 | Free | Free | Linear | L | None | Recombinant slow-release TNF α-derived peptide | Tumor growth inhibitor and anti-angiogenic | Blood sample collected after0.5-24 hours after the injection of peptide | 5mg/kg | 13.11 ±1.49 | BALB/c mice plasma proteases | LC/MS | BALB/c mice plasma (Dose i/v injected) | in vivo | None | None | Growth 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% | |||
| 25625650 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 0.25-84 hours | 0.6mg s/c injected | 12 ±2.8 | Cat blood proteases | ELISA | Healthy cat blood (Dose s/c injected) | in vivo | None | None | Insulin 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 | |||
| 24139844 | 2013 | Conjuagte 2(conjugates of 4-aminocyclophosphamide (4-NH2-CPA)) | 6 | Succinylation | Amidated CPA | Linear | L | None | Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA) | Anti-cancer | Not mentioned | Not mentioned | 12 | PSA(Prostate-specific antigen ) | HPLC | Conjuagte 2+PSA(Prostate-specific antigen) | in vitro | None | None | pEC50-8.59 ±0.9minutes, Emax 9.30 ±0.26nmol/well | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | >12 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 1329046 | 1992 | [Psi13,14]BN [Bombesin antagonist] | 14 | Free | Amidation | Linear | L | Pyr=Pyro-glutamine | Bombesin analogue | Growth inhibitors | 0-1080 minutes | 50μM | 646 | Degradative enzymes or SCLC cell line proteases | RP-HPLC | SCLC cell line NCI-H345 | in vitro | None | None | IC50= 30nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 12.6 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (5%) + heat inactvation | in vitro | None | None | Not mentioned | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 11.5 | Proteases from Heat inactivated calf serum | HPLC | Heat inactivated calf serum + 1μM catropril | in vitro | None | None | Not reported | |||
| 8218482 | 1993 | YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer) | 5 | Free | Free | Linear | L | Peptide covalently attached to Isocyanate containing polyurethane prepolymer | Synthetic RGD containing peptide | Cell attachment property | Not mentioned | Not mentioned | 11.3(Half life of 2nd phase) | Proteases from mouse bood | HPLC | Mouse blood | in vivo | None | None | Not reported | |||
| 21210710 | 2011 | Linear chlorotoxin(CTX) | 36 | Free | Free | Linear | L | N-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 27 | Scorpion venom | Identify tumor foci with high sensitivity | 24 hours | 50μl of 40μM | 14 | Mice serum proteases | Imaging system to measure fluorescent intensity | Intravenous injection in two month old wild-type C57BL/6 mice | in vivo | http://www.drugbank.ca/drugs/DB00140 | None | Fluorescent efficiency (cm2) in the tumor compared with control mice=2.49 ±1 | |||
| 21210710 | 2011 | Cyclic chlorotoxin(CTX) | 43 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35) | L | N-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 28 | Analog of CTX | Identify tumor foci with high sensitivity | 24 hours | 50μl of 40μM | 11 | Mice serum proteases | Imaging system to measure fluorescent intensity | Intravenous injection in two month old wild-type C57BL/6 mice | in vivo | http://www.drugbank.ca/drugs/DB00141 | None | Fluorescent efficiency (cm2) in the tumor compared with control mice=3.3 ±1.81 | |||
| 38789061 | 2024 | Liraglutide (Lymph cannulated) | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Lymph 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 hr | 2 mg/kg | 12.61 ± 5.45 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide (Lymph cannulated) | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Lymph 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 hr | 1 mg/kg | 10.26 ± 6.51 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38340726 | 2024 | A1L35HR2m-Chol | 114 | Conjugation 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 terminal | Linear | L | None | fusion protein of A1 and HR2m | Antiviral (Inhibits Coronaviruses) | N.A. | 5 mg/kg | 10.6 | Balb/c mice serum protease | N.A. | Balb/c mice trachea tissue homogenate | In Vivo | None | None | A1L35HR2m was highly potent in inhibiting SARS-CoV-2 infection with an IC50 value of 27 nM | |||
| 38293540 | 2024 | GLP-ABD-XTEN144 | 257 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (144 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 12.9 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN144 has a Kd value of only 5.50 nM | |||
| 38236561 | 2024 | Cotadutide | 29 | Free | Free | Linear | L | palm-Glu-OH conjugated at Lys9 side chain | Synthetic | Dual GLP-1 and Glucagon (GCG) Receptor agonist | N.A. | 20 to 600 μg | 13.3 | N.A. | N.A. | N.A. | In Vivo | None | None | N.A. | |||
| 37449781 | 2023 | NCL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood 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 h | 5 μg/μL | 11.4 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 37449781 | 2023 | 2F-CL30 | 230 | Polysarcosine = poly(N-methyl glycine) | Free | Linear | L | fluorescently labeled with Atto647N, polysarcosine-block-poly(S-ethylsulfonyl-l-cysteine) | synthetic | Improve the therapeutic profile of hydrophobic drugs, reduce or completely avoid protein corona formation | Blood 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 h | 5 μg/μL | 11.3 | C57BL/6 mice plasma protease | Fluorescence spectrophotometry | C57BL/6 mice plasma | In Vivo | None | None | Not mentioned | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 14 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| 36630826 | 2023 | Ex-PEGRh(4.4 ± 1.1nm) | 39 | Free | PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 12.1 ± 1.0 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten 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/kg | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 (nM) = 1.3 ± 0.2 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.3 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2.0 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.2 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.8 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 12.9 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 12.1 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 22 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 13.6 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 1 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 14.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 14.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 31 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, NMeS = N- methyl-L-serine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 12 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 50.3 | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 736.6 ± 12.3 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 738.6 ± 9.7 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 777.0 ± 10.2 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment 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 22 | 1 mg | 10.4 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal , Amidation | Linear | L | None | GLP-2 analogue | Treatment 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 22 | 1 mg | 11.7 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36142749 | 2022 | PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | opioid–neurotensin hybrid peptide | Analgesic | 37°C for 24 h | 50 μg/mL | 11.36 | N.A. | LC-MS | 1M NaOH | In Vitro | None | None | EC50 = 79 nM (potency at mu opioid receptor) | |||
| 36075899 | 2022 | S-20-1 | N.A. | N.A. | N.A. | Cyclic | L | Modified by adding negative charge | Synthetic | Antiviral (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 h | 50 mg/kg | 14.53 (Terminal Elimination Half Life) | C57Bl/6 mice plasma protease | LC-MS/MS | C57BL/6 mice plasma | In Vivo | None | None | IC50 (μM) = 0.8 in HUH 7 cells | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 20 nmol/kg | 10.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18059 pmol/kg | 12.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18058 pmol/kg | 10.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18052 pmol/kg | 12.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | N.A. | 200 nmol/kg | 11 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (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 | |||
| 35688476 | 2022 | PEG-hUCN1 | 40 | Free | Amidation | Linear | L | Insertion of a cysteine residue at position 31 for pegylation PEG20 acetamide | Human UCN1 derivative | Treating Autoimmune disease | N.A. | 0.3 mg/kg | 13 | C57Bl/6J mice plasma protease | Laser capture/mass spectrometry | C57BL/6J mice plasma | In Vivo | None | None | At 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 | |||
| 35677307 | 2022 | PEG10k-rhG-CSF | 175 | Free | Free | Linear | L | PEG10K-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168h | 1.0 mg/kg | 13.05 ± 0.45 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35582852 | 2022 | CP | 8 | Free | PNAM37 linked through NH2 group | Cyclic(N-C terminal bond) | Mix | D-leucine at position 1 and 3 | Synthetic | Drug delivery vectors | Blood 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 administratio | 1 μCi | 14.6 ± 2.9 (Elimination Half Life) | Rats plasma protease | Liquid scintillation counter | Rats plasma | In Vivo | None | None | For concentrations of 1 mg/mL CP , cell viabilities drop to about 75% for the 4T1 cell line | |||
| 35414877 | 2022 | B_1275.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 643(Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 1209 | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood 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 infusion | 0.125 mg/kg | 10.5 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood 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 infusion | 0.25 mg/kg | 13.16 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 35177945 | 2022 | (Ala13)apelin-13 | 13 | Free | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 10.3 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.74e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Ala13)apelin-13 | 13 | pGlu = Pyroglutamate | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 11.1 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 7.68e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Tyr13)apelin-13 | 13 | pGlu = Pyroglutamate | Tyr13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 12.2 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.48e-008 (In vitro insulin secretion) | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(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) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 11.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(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) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 14 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(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) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 12.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(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) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 12.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 88.23 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 11.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35807558 | 2022 | [MeArg35]PYY3−36 | 34 | Free | Methylated Arg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 620 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeGln34]PYY3−36 | 34 | Free | Methylated Gln34 at C terminus | Linear | L | Methylated Gln34 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 890 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 0.40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoArg35]PYY3−36 | 34 | Free | β-homoArg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 680 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 6300 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 34707178 | 2021 | PYY3-36 analogues 2 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 4 (C18 diacid-γGlu-2xAdo) | Derived from PYY | Antiobesity | Blood 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 dosing | 15 nmol/kg | 14 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 10 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 7 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 9 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 12 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 40 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 9 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 11 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 11 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 1.3 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 11 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 13 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 16 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 39 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 50 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 120 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34163352 | 2021 | NOPT | 16 | OPT substituted with an N-methyl proline at position 1 | Free | Linear | L | None | Derived from OPT | Binds To Pser68-Plm | Aliquots of 50 μl were collected at different time points (0–48 h) | 300 μM | 14.9 | Human serum protease | Mass spectrometry | Human serum | In Vitro | None | None | N.A. | |||
| 33940058 | 2021 | OPBP-1@TMC | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-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/kg | 14.55 ± 1.43 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33918853 | 2021 | HFn-PAS/DOX | 235 | Free | 15aa linker, enzyme cleavable site, PAS(40), 5 aa flexible linker conjugated at C terminus | Linear | L | None | Synthetic | Antitumor | Blood 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 °C | 3.0 mg/kg | 14.96 ± 0.29 | SD rats serum protease | Fluorescence spectrometry | SD rats serum | In Vivo | PDB id: 3AJO | None | IC50 (μg mL−1) = 0.38 ± 0.09 | |||
| 32078672 | 2020 | rFVIIIFc | 865 | Free | IgG1 Fc | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 13.2 | VWF Het mice plasma protease | chromogenic activity assays | VWF Het mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32858124 | 2020 | Cmpd# 10 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.2 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6 | |||
| 32858124 | 2020 | Cmpd# 14 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9 | |||
| 32803073 | 2020 | Pal-Rb | 169 | Free | Free | Linear | L | Conjugation of palmitic acid at AzF, biotinylated labelling, , (AzF) was incorporated into the position 126 on the repebody followed by lipid conjugation | Synthetic | Antitumor | Blood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h | 10 mg/kg | 10.7 (Elimination Half-Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB ID: 4J4L | None | The 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. | |||
| 32608185 | 2020 | 125I-M-E5 | 22 | Free | Tyrosine (Y) residue was added to E5 sequence and 125I was added | Linear | L | None | Synthetic | Anticancer (Treatment of Acute Myeloid Leukemia) | N.A. | 50 µg/g | 14.53 ± 6.04 | Rats plasma protease | Gamma counter | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4196105/#sec10 | None | The 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 | |||
| 32404523 | 2020 | PEG40-NC | 34 | Free | Free | Linear | L | PEGylation at Asn637 in native gp41 | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood 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/kg | 10.39 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 35496622 | 2020 | Lixisenatide 1a | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.2 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.19 ± 0.02 for Lixisenatide 1a (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1d | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.085 ± 0.021 for Lixisenatide 1d (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1g | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 11.9 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.59 ± 0.16 for Lixisenatide 1g (in vitro GLP-1 receptor activation potency) | |||
| 32133341 | 2020 | Apamin based analogs 3 | 25 | Free | Free | Cyclic (C1-C11, C3-C15) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 12.8 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.65 ± 0.18 | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.025 mg/kg | 782 ± 365 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 11.7 ± 1.4 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| N.A. | 2020 | Ac-(06-34-18) (HomoArg5) | 12 | Acetylation | Free | Linear | L | HomoArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 10.7 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 64 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 HomoArg5 | 12 | Acetylation | Free | Linear | L | HomoArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 12.2 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 19.7 | |||
| 31654685 | 2019 | Repebody-fused GLP-1 in complex with HSA | 50 | Repebody | GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice 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 abdominalis | 25 nmol/kg | 10.7 (Terminal Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/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 | |||
| 31443181 | 2019 | FcRn | 365 | Free | Free | Linear | L | None | Isolated from human gastric juice | Role in extending the serum half life of therapeutic antibodies | Blood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrs | N.A. | 10.6 | PBMC lysate protease (African American) | LC-MS/MS | PBMC lysate (African American) | In Vitro | Uniprot id: P55899 | None | N.A. | |||
| 31443181 | 2019 | FcRn | 365 | Free | Free | Linear | L | None | Isolated from human gastric juice | Role in extending the serum half life of therapeutic antibodies | Blood collection at 0, 1.5, 3, 4.5, 6, 7.5, 9, 12, 15, 18, 21, 24, 27, 30, 33, 36 hrs | N.A. | 11.6 | PBMC lysate protease (African American) | LC-MS/MS | PBMC lysate (African American) | In Vitro | Uniprot id: P55899 | None | N.A. | |||
| 31453257 | 2019 | Pept. A | N.A. | Free | Free | Cyclic | L | N.A. | N.A. | Therapeutic agent against a CNS-related disorder | Blood (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/kg | 14.3 ± 5.5 (Terminal Half Life) | göttingen Minipig Csf Lumbar Protease | LC-MS/MS | Göttingen minipigs CSF lumbar | In Vivo | None | None | N.A. | |||
| 31235532 | 2019 | CNP-38 | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | 4 days | 100 μg/ml | 12.6 ± 3.9 | Recombinant human NEP protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 100 (NPR-C Affinity) | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 12.9 ± 4.6 | Sham rats plasma protease | LC–MS/MS | Sham rats plasma | In Vivo | None | None | N.A. | |||
| 31156041 | 2019 | AD-114-Im7 PEG 30K | 118 | Free | lm7-PEG30K | Linear | L | None | Fusion protein of AD-114 with lm7 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 3 mg/kg | 11.85 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 0.7 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected at 15, 30 min, 1, 2, 3, 4, 8, 12,18, 24, 36, 48 and 72 h post dosing | 10 mg/kg | 10.25 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood 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/kg | 10.2 ± 3.9 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 1 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood 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 administration | 17.4 µ/kg | 11.4 ± 1.0 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood 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 intravenous | 17.4 µ/kg | 12.9 ± 1.0 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 30606721 | 2019 | BCY-B5 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | 11.5 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 11 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 10 mg/kg | 11 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPKEG80 | 400 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 12.4 ± 0.1 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPKEG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 12.9 ± 0.2 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPKEG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 12.0 ± 0.4 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 17 nM for GLP1-VPKEG120 | |||
| 30504081 | 2019 | VPKDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 10.8 ± 0.2 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPGAG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 10.6 ± 1.6 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 12.4 ± 0.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPKDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =K, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 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 vein | 300 μM | 11.8 ± 1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30565900 | 2018 | DOX@PLEPMPss-cRGD | 3 | PCL-PEG | Free | Cyclic (N-C terminal end) | L | None | Synthetic | Anticancer | The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h) | 2 mg/kg | 11.81 ± 0.67 (T1/2b) | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1 | |||
| 30565900 | 2018 | DOX@Cu-PLEPMPss-cRGD | 3 | PCL-PEG | Free | Cyclic (N-C terminal end) | L | None | Synthetic | Anticancer | The plasma was collected after injection at predetermined time points (1, 3, 6, 12, and 24 h) | 2 mg/kg | 12.20 ± 0.73 (T1/2b) | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | The IC50 value (i.e., the concentration resulting in 50% cell inhibition) forDOX@Cu-PLEPMPsscRGD micelles was 2.884 µg mL−1 | |||
| 30496575 | 2018 | rhIFN-λ1-CTPON | 218 | Free | Human chorionic gonadotropin β subunit carboxyl-terminal peptide (CTP) and an N-glycosylation sequence linked to its C-terminus via linker | Linear | L | None | Recombinant human interferon-λ1 derivative | Antiviral, Antiproliferation, And Nk Cell Cytotoxicity-Promoting Activities | Venous blood was collected at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h post-injection | 40 μg/kg | 10.326 ± 0.87 | Mice blood protease | ELISA | Mice blood sample | In Vivo | None | None | Antiviral activity of the purified rhIFN-λ1 expressed by CHO cells was 2.5 × 105 IU/mg | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | At 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 eyeball | 50 nmol/kg | 10.8 ± 0.8 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin | 50 nmol/kg | 12.9 ± 3.6 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood 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 impairment | 2.2 mg/kg | 14.1 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Mild Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 30 μg | 11.43 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 100 μg | 12.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 150 μg | 10.97 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29799205 | 2018 | 5b | 39 | Free | Free | Linear | L | X4 = structure given in paper | GLP-1 analogs | Antidiabetes | Serial 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 h | 50 nmol/kg | 11.0 ± 1.2 | SD rats plasma protease | LC-MS/MS. | SD rats plasma | In Vivo | None | None | N.A. | |||
| 29732120 | 2018 | Cilen | 5 | Free | Free | Macrocyclic (N-C terminal end) | Mix | Methylation at Phenylalanine (D-form) | Synthetic | Glioblastoma therapy | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 12 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 value of 11 shows that 11 is poorer than Cilen | |||
| 29329072 | 2018 | Compound 32 | 8 | Acetylation | Amidation | Linear | L | N(benzyl)Gly modfication at position 4 | NMU-analogs | Regulation Of Feeding Behavior, The Stress Response And Nociception | 37 °C | 112 µM | 837.4 ± 27.8 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 172.2, IC50(nM) = 83.1 for hNMUR1 and EC50(nM) = 1278, IC50(nM) = 1019 for hNMUR2 | |||
| N.A. | 2018 | TRAIL-ASPD_F335D | 347 | Free | C-type lectin domain of human SP-D joined with Strep-tag II using linker | Linear | L | Phe355 -> Asp355 modification | Trail-SPD Fusion Protein | Therapeutic, diagnostic and/or research applications | Serum samples were collected after several time points (predose, 5 min., 30 min., 2H, 6H and 24H) | 10 μg | 14 | CD1 mice serum protease | ELISA | CD1 mice serum | In Vivo | None | EP 17197297 A | Five hours of co-incubation of primary human hepatocytes with trimeric TRAIL-ASPD_F335D together with chemotherapeutic drugs induced no caspase activity (E) | |||
| 28821462 | 2017 | LCFN144 | 183 | Free | Fusing the XTEN peptide of 144 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 11.3 ± 1.0 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28821462 | 2017 | LCFN288 | 183 | Free | Fusing the XTEN peptide of 288 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 10.2 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28714475 | 2017 | Tag | 7 | Fluorescein (F) | Amidation | Linear | L | Lys4 linked with Palm fatty acid | Synthetic | Increases Half Life | N.A. | 0.25 mg/kg | 12.3 ± 0.4 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 220±30 for rat albumin | |||
| 28356733 | 2017 | SCD | 32 | Free | Chitosan-modified SeNP (SC) | Linear | L | None | Peptide-conjugated selenium nanoparticles | Antidiabetes | Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing | 1 mg/kg | 14.12 | DB/DB mice orbital blood protease | LC-MS/MS | DB/DB mice orbital blood sample | In Vivo | None | None | IC50 of SC for INS-1 cells was 66.10 μM | |||
| 28281868 | 2017 | HSA-eTGFBR2 | 697 | Free | eTGFBR2 fused at the C-terminal of HSA | Linear | L | None | Synthetic | Neutralize TGF-Β1 activity | Blood samples were collected 5 min, 15 min, 30 min, 1 h, 2 h, 6 h,12 h, 24 h | 3 nmol/kg | 11.84 | Mice serum protease | Human TGF-b RII Duo Set ELISA | Mice serum | In Vivo | pdb id: 4P7U, 7DJN | None | KD = 1.42* 10-8M of HSA-eTGFBR2 for TGF-B1 | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Bicarinalin 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 | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [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. | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 12.2, 3, 8.7, 0.45, 24.4 for E.hirae, S.aureus, MRSA, S.xylosus, B.subtilis respectively | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [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 | |||
| 32263229 | 2016 | iT-P/PTX NPs | 5 | Free | TPGS(D-a-tocopherol polyethylene glycol succinate) linked with poly(lactide) using disulfide linkage, cRGD further conjugated to NP surface | Cyclic (RGDfC) | Mix | D-Phe at position 4 | Synthetic | Anticancer | Blood 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/ kg | 12.68 ± 0.81 | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | IC50 = 1.90 ± 0.28 mg/mL incubated with A2780 cell | |||
| 26808305 | 2016 | αAnalogue | 37 | Fatty acid moiety attached to Ser1 at N terminal | Amidation | Cyclic (Disulfide Bridge Between Positions 2 And 7) | L | None | CGRP analogue | Vasodilatory effect | Blood (200 µl) was sampled from vena sublingualis from anaesthetised rats at pre-dose and at 0.5, 1, 3, 7 and 24 h post dosing | 151 nmol/kg | 10.2 ± 0.9 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | https://sci-hub.st/10.1126/science.2994212, | None | N.A. | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 5 | 13 | R5( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 7 | 13 | R7( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 9 | 13 | R9( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26806490 | 2016 | CTP-IFN-CTP | 221 | CTP ( 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)) | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 13.4 ± 1.5 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | None | None | Specific antiviral bioactivity (U ng−1) = 44 ± 3, Specific antiproliferative bioactivity (U ng−1) = 9 ± 1 | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 10.16 | Carboxy-Peptidase A | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with CPA (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 12.38 | Trypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Trypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 14.28 | Pepsin | Mass spectrometry | Gastric fluid solution (pH 1.2) with Pepsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 1.5 mg/kg | 12.76 ± 2.06 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 181 | 1.5 mg/kg | 17.01 ± 6.91 | Monkeys serum protease | Sandwich ELISA | Monkeys serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) |