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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 10495424 | 1999 | MART-127 €“35 | 9 | Free | Free | Linear | L | None | Synthetic | Immunogenic peptides | Not given | 1 µM | 22 | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 0.5 µM | |||
| 10495424 | 1999 | PEG-MART-1 | 9 | Free | Pegylation | Linear | L | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is >35 µM | |||
| 10495424 | 1999 | D-MART-1 | 9 | Free | Free | Linear | Mix | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | Not tested | |||
| 10495424 | 1999 | Glyco-MART-1 | 9 | Asn(β-D-GlcNHAc) | Free | Linear | L | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | Not tested | |||
| 10495424 | 1999 | Cap-MART-1 | 9 | Acetylation | Amidation | Linear | L | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 65 µM | |||
| 10495424 | 1999 | N-MART-1 | 9 | Acetylation | Free | Linear | L | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 35 µM | |||
| 10495424 | 1999 | C-MART-1 | 9 | Free | Amidation | Linear | L | None | Synthetic | Immunogenic peptides | Not given | Not given | Stability increased | Human plasma proteases and proteases of VMM5 cytotoxic T-lymphocyte | Not mentioned | VMM5 cytotoxic T-lymphocyte line incubated in human plasma | in vitro | None | None | IC50 for inhibition of binding of a standard peptide to HLA-A*0201 molecules is 7 µM | |||
| 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 | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 18.73 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch2 | in vitro | None | None | Not reported | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 4.62 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch3 | in vitro | None | None | Not reported | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 7.29 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch4 | in vitro | None | None | Not reported | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=4 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=7 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. Luteus ATCC 9342 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9343 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3.12 µg/ml for M. Luteus ATCC 9344 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6 µg/ml for M. Luteus ATCC 9345 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for S. Aureus ATCC 6538 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for S. Aureus ATCC 6538 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=19 µg/ml for S. Aureus ATCC 6539 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for S. Aureus ATCC 6540 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for S. Aureus ATCC 6541 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for S. Aureus ATCC 6542 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for S. Aureus ATCC 6543 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 µg/ml for S. Aureus ATCC 6544 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3.12 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3.12 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=2 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | Not reported | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for MRSA SR 1550 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=50 µg/ml for MRSA SR 1551 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=100 µg/ml for MRSA SR 1552 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=50 µg/ml for MRSA SR 1553 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=>100 µg/ml for MRSA SR 1554 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=42 µg/ml for MRSA SR 1555 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=38 µg/ml for MRSA SR 1556 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=16 µg/ml for MRSA SR 1557 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=>100 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 612 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 613 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | Not reported | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=23 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=31 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=21 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=19 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=4 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=20 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=5 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=17 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=31 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for C. albicans ATCC 36232 | |||
| 10773009 | 2000 | TX14(A) | 14 | Free | Free | Linear | Mix | None | Synthetic derivative of prosaposin | Neurotrophic factor | 9 minutes | Not mentioned | 4.2 ±0.3 | Rat serum proteases | Radioactivity measured with a gamma counter | Injected in jugular vein of male Sprague-Dawley rats | in vivo | None | None | ED50=1.00 ±0.11ng/ml | |||
| 10773009 | 2000 | TX15-2 | 15 | Free | Free | Linear | Mix | None | Synthetic derivative of prosaposin | Neurotrophic factor | 9 minutes | Not mentioned | 2.5 ±0.3 | Rat serum proteases | Radioactivity measured by a gamma counter | Injected in jugular vein of male Sprague-Dawley rats | in vivo | None | None | ED50=1.00 ±0.09ng/ml | |||
| 10541299 | 1999 | Epoetin | 166 | Free | Free | Cyclic | L | Three N-linked carbohydrate chains | Recombinant human erythropoietin | Stimulates erythropoiesis | Not mentioned | Not mentioned | 8.5 ±2.4 | Human blood proteases | ELISA | Subcutaneously injected into patients with end-stage renal failure | in vivo | http://www.drugbank.ca/drugs/DB00016 | None | Not reported | |||
| 10541299 | 1999 | Novel erythropoiesis stimulating protein (NESP) | 166 | Free | Free | Cyclic | L | Five N-linked carbohydrate chains | Hyperglycosylated analogue of recombinant human erythropoietin | Stimulates erythropoiesis | Not mentioned | Not mentioned | 25.3 ±2.2 | Human blood proteases | ELISA | Subcutaneously injected into patients with end-stage renal failure | in vivo | http://www.drugbank.ca/drugs/DB00017 | None | Not reported | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 12.7 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 2.6 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 22 | Human blood proteases | HPLC | Injected in humans | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 10670753 | 1999 | Human thyrotropin-releasing hormone (TRH)-associated peptide 3 (hTAP-3) | 9 | Free | Free | Linear | L | None | Product of proteolysis of preproTRH | Serum hTAP-3 concentration was increased in patients with hyperthyroidism | 15 min | Not mentioned | 3.5 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | None | None | Not reported | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | Not mentioned | 10 ±1 | Angiotensin-converting enzyme | Radioimmunoassay and HPLC | Blood sample of normotensive Sprague-Dawley rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | 10 ±1 | Angiotensin-converting enzyme | Radioimmunoassay and HPLC | Blood sample of anesthetized spontaneously hypertensive rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | 9 ±1 | Angiotensin-converting enzyme | Radioimmunoassay and HPLC | Blood sample of mRen-2 transgenic rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~11 ±1 | Angiotensin-converting enzyme and losartan(AT1 antagonist) | Radioimmunoassay and HPLC | Blood sample of normotensive Sprague-Dawley rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~11 ±1 | Angiotensin-converting enzyme and losartan(AT1 antagonist) | Radioimmunoassay and HPLC | Blood sample of anesthetized spontaneously hypertensive rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~14 ±1 | Angiotensin-converting enzyme and losartan(AT1 antagonist) | Radioimmunoassay and HPLC | Blood sample of mRen-2 transgenic rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~60 ±1 | Angiotensin-converting enzyme and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of normotensive Sprague-Dawley rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~44 ±1 | Angiotensin-converting enzyme and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of anesthetized spontaneously hypertensive rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~29 ±1 | Angiotensin-converting enzyme and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of mRen-2 transgenic rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~45 ±1 | Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of normotensive Sprague-Dawley rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~49 ±1 | Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of anesthetized spontaneously hypertensive rat | in vivo | None | None | Not mentioned | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~40 ±1 | Angiotensin-converting enzyme,losartan(AT1 antagonist)and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of mRen-2 transgenic rat | in vivo | None | None | Not mentioned | |||
| 9806949 | 1998 | MEN 11420 | 6 | Glycosylation | Free | Cyclic | L | Dpr-2,3-Diaminopropionic acid | MEN 10627 | Tachykinin NK2 receptor antagonist | Not reported | Not mentioned | 44 ±3 | Not mentioned | HPLC | Rat blood plasma | in vivo | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 8 | γ-secretase | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 1 | γ-secretase (protease) Lactacystin(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 10 | γ-secretase (protease) ALLN(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 10611139 | 1999 | Hexarelin | 6 | Free | Amidation | Linear | Mix | 2me-2-methyl(tryptophan) | Analog of GHRP-6 | Peptidyl growth hormone causing GH releasing effect. | Not reported | 10 to 25 iu of oxytocin | 75.9 ±9.3 | Blood proteases | LC-MS/MS | Intravenous injection,Blood sample from male Sprague-Dawley rats | in vivo | None | None | Not mentioned | |||
| 10611139 | 1999 | Hexarelin | 6 | Free | Amidation | Linear | Mix | 2me-2-methyl(tryptophan) | Analog of GHRP-6 | Peptidyl growth hormone causing GH releasing effect. | Not reported | 5 µg/kg | 71.9 ±11.2 | Blood proteases | LC-MS/MS | Intravenous injection,Blood sample from male Sprague-Dawley rats | in vivo | None | None | Not mentioned | |||
| 10611139 | 1999 | Hexarelin | 6 | Free | Amidation | Linear | Mix | 2me-2-methyl(tryptophan) | Analog of GHRP-6 | Peptidyl growth hormone causing GH releasing effect. | Not reported | 10 µg/kg | 61.4 ±9.5 | Blood proteases | LC-MS/MS | Intravenous injection,Blood sample from male Sprague-Dawley rats | in vivo | None | None | Not mentioned | |||
| 10611139 | 1999 | Hexarelin | 6 | Free | Amidation | Linear | Mix | 2me-2-methyl(tryptophan) | Analog of GHRP-6 | Peptidyl growth hormone causing GH releasing effect. | Not reported | 50 µg/kg | 57.0 ±9.1 | Blood proteases | LC-MS/MS | Intravenous injection,Blood sample from male Sprague-Dawley rats | in vivo | None | None | Not mentioned | |||
| 10647619 | 2000 | TP 850 | 10 | Free | Free | Linear | Mix | 4-aminobutyric acid (Aba) | Modified fibrin α chain N-terminal peptide | Blood Coagulation | Not reported | 11 to 25 iu of oxytocin | 4 | Blood proteases | Radiolabelling and HPLC | Intravenous injection,Blood sample of rabbit | in vivo | None | None | Platelet aggregation inhibition, IC50=236μm for dog and IC50=167μm for rabbit. | |||
| 10871321 | 2000 | BK1-5 | 5 | Free | Free | Linear | L | None | Metabolite of bradykinin | Not mentioned | Not reported | 106 cpm/200μl/mouse | ~90 | Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidase | HPLC-ESI-MS | Intravenous injection of Bradykinin,Human blood sample | in vivo | None | None | Not mentioned | |||
| 10871321 | 2000 | Bradykinin | 9 | Free | Free | Linear | L | None | Human blood plasma | Cardioprotective effects | Not reported | 106 cpm/200μl/mouse | Not measured as peptide degraded rapidly<30 approx. | Aminopeptidase P,Dipeptidyl-peptidaseIV,KininaseII,KininaseI and neutral endopeptidase | HPLC-ESI-MS | Human blood sample | in vivo | None | None | Not mentioned | |||
| 10454085 | 1999 | Oxytocin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Hypothalamus | Involved in aiding mechanical clearance mechanism and improving fertility | 60 minutes | 90mg | 6.78 | Blood protease | Radioimmunoassay | Intravenous injection of oxytocin in normal mares | in vivo | None | None | Prostaglandin F metabolite(PGFM) release on administeration of 10 iu of oxytocin= 18.48 ±3.62 pg/ml | |||
| 10454085 | 1999 | Oxytocin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Hypothalamus | Involved in aiding mechanical clearance mechanism and improving fertility | 60 minutes | 180mg | 6.78 | Blood protease | Radioimmunoassay | Intravenous injection of oxytocin in normal mares | in vivo | None | None | Prostaglandin F metabolite(PGFM) release on administeration of 25 iu of oxytocin= 20.09 ±3.29 pg/ml | |||
| 10544005 | 1999 | YIGSR | 5 | Free | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | <1 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 1.5μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50% | |||
| 10544005 | 1999 | PEG5000 -YIGSR | 5 | Pegylated by addition of PEG5000 | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 2.2 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx. | |||
| 10544005 | 2000 | PEG12,000 -YIGSR | 5 | Pegylated by addition of PEG12,000 | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 2.5 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50% | |||
| 8910426 | 1996 | LL:36 €“45 | 10 | Free | Free | Linear | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 17 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | No cell lysis done by this peptide | |||
| 8910426 | 1996 | LALF-10 (38 €“45) | 12 | Free | Free | Cyclic (C2-C11) | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 77 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | LD50=2.58 mg/ml | |||
| 8910426 | 1996 | LALF-14 (36 €“47) | 16 | Free | Free | Cyclic (C2-C15) | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 84 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | LD50=2.33 mg/ml | |||
| 9067297 | 1996 | E-2078 [N-methyl-Tyr1, N-methyl-Arg7-D-Leu8] Dyn A (1 €“8) ethylamide] | N.A. | Methylation | Ethylamide | Linear | Mix | Methylation on Arg7 and Tyr1 | Dynorphin A (1 €“ 8) analog | Analgesic | Not reported | 10 mg/kg | 44 | Monkey blood proteases | MALDI-MS | Rhesus monkey blood plasma (Intravenous) | in vivo | 7479294 | None | Not available | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 15, 30, 45, and 60min | 0.10mg/kg | 1 (t1/2 α) | Rat blood plasma proteases | HPLC-MS | Intravenous administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min | 0.10mg/kg | 13 (t1/2 α) | Dog blood plasma proteases | HPLC-MS | Intravenous administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 4 (t1/2 α) | Rabbit blood plasma proteases | HPLC-MS | Intravenous administered to Rabbit | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 5 (t1/2 α) | Monkey blood plasma proteases | HPLC-MS | Intravenous administered to Monkey | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 15, 30, 45, and 60min | 0.10mg/kg | 15 (t1/2 β) | Rat blood plasma proteases | HPLC-MS | Intravenous administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min | 0.10mg/kg | 64 (t1/2 β) | Dog blood plasma proteases | HPLC-MS | Intravenous administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 64 (t1/2 β) | Rabbit blood plasma proteases | HPLC-MS | Intravenous administered to Rabbit | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 68 (t1/2 β) | Monkey blood plasma proteases | HPLC-MS | Intravenous administered to Monkey | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 5 mg/kg | 73 (t1/2 β) | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min | 5 mg/kg | 45 (t1/2 β) | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 5 mg/kg | 51 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 50 mg/kg | 80 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 300 mg/kg | 99 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 500 mg/kg | 122 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 1000 mg/kg | 204 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 5 mg/kg | 51 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 5 mg/kg | 74 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 50 mg/kg | 80 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 50 mg/kg | 71 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 300 mg/kg | 99 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 300 mg/kg | 100 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 5 mg/kg | 45 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 5 mg/kg | 44 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 50 mg/kg | 48 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 50 mg/kg | 50 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 300 mg/kg | 75 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 300 mg/kg | 76 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 9062685 | 1997 | [pGIu4,Cyt6]AVP(4-9) | 6 | Free | Amidation | Linear | L | pGlu = pyroglutamate | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 10 ng/kg | 40 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive 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. | |||
| 9062685 | 1997 | [Cys6]AVP(5-8) | 4 | Free | Free | Linear | L | At 2 position cystine is replaced by cysteine | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 1 ng/kg | 10 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive 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. | |||
| 9062685 | 1997 | No.302 | 6 | Free | Amidation | Linear | L | pGlu = pyroglutamate | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 0.1, 1 and 10ng/kg | 9 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive 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. | |||
| 9062685 | 1997 | Analogue of [Cys6]AVP(5-8) | 4 | Free | Free | Linear | L | None | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 10 ng/kg | 223 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive 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. | |||
| 9357069 | 1997 | [D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P | 11 | Free | Amidation | Linear | Mix | None | Substance P | Neuropeptide growth factor antagonist | upto 360 minutes | 12 µg/g body weight of mice | 45.9 (terminal t1/2) | Mice blood proteases | RP-HPLC | Intraperitonial injection to Nu/Nu mice | in vivo | http://www.abcam.com/d-arg1d-phe5d-trp79leu11-subs | None | Not reported | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 0.8 ±0.1 (t1/2 fast phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats treated with carvedilol | in vivo | None | None | ANP 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. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 0.9 ±0.1 (t1/2 fast phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats | in vivo | None | None | ANP 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. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 7.7 ±0.8 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats treated with carvedilol | in vivo | None | None | ANP 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. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 4.9 ±0.5 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats | in vivo | None | None | ANP 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. | |||
| 9589822 | 1998 | Eptifibatide | 7 | Mpr=mercaptopropionyl | Amidation | Cyclic (disulfide bridge between cysteine and mercaptopropionyl) | L | None | Venom of pygmy rattlesnake | Antithrombotic | 1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours | 135 μg/kg | 1.13 ±0.17 (t1/2 termination) | Human blood plasma proteases | HPLC | Intravenous injection to Human | in vitro | http://www.prospecbio.com/Eptifibatide_11_124/ | None | Not tested | |||
| 9589822 | 1998 | Eptifibatide | 7 | Mpr=mercaptopropionyl | Amidation | Cyclic (disulfide bridge between cysteine amide and mercaptopropionyl) | L | None | Venom of pygmy rattlesnake | Antithrombotic | 1.5, 2, 4, 6, 8, 12, 16, 24, 36, 48, 60, and 72 hours | 135 μg/kg | 5 ±2.5 (t1/2 distribution) | Human blood plasma proteases | HPLC | Intravenous injection to Human | in vitro | http://www.prospecbio.com/Eptifibatide_11_124/ | None | Not tested | |||
| 9932163 | 1998 | Cemadotin-HCl | 5 | Free | Free | Linear | L | None | Synthetic analogue of Dolastatin 15 | Antimitotic | 24 hour | 10 - 27.5mg | 10 | Human blood proteases | Radioimmunoassay | Intravenous administration to human | in vivo | None | None | Cancer patient was administered with Cemadotin for 24 hours intravenously at dose of 10mg. Reduction in liver metastasis was observed by sonographic examination. | |||
| 10354413 | 1999 | Thioimreg compound 11 | 3 | Free | Free | Linear | L | Peptide bonds at position 1,2 was replaced by thioamide linkages | Thioanalogue of natural Imreg | Immunostimulant | 3.5 hours | Not given | 46 | Rat blood proteases | HPLC | Rat whole blood | in vitro | None | None | 125 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 | |||
| 10354413 | 1999 | Imreg | 3 | Free | Free | Linear | L | None | Human leucocyte | Immunostimulant and in clinical trial to treat AIDS | 3.5 hours | Not given | <1 | Rat blood proteases | HPLC | Rat whole blood | in vitro | None | None | Immunophenotyping 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 | |||
| 10354413 | 1999 | Thioimreg compound 8 | 3 | Free | Free | Linear | L | Peptide bonds at position 2,3 was replaced by thioamide linkage | Thioanalogue of natural Imreg | Immunostimulant | 3.5 hours | Not given | >180 | Rat blood proteases | HPLC | Rat whole blood | in vitro | None | None | A weak in vitro induction of T (PHA) and B (PWM) cell proliferation (1.5 to 2-fold increase) by the thioanalogues | |||
| 10573295 | 1999 | Enkephalin | 6 | Free | Amidation | Linear | L | None | Natural (Human brain) | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | 30 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | None | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para chlorination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para bromination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para florination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para iodination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin | 6 | Free | Amidation | Linear | L | None | Natural (Human brain) | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Hydroxylation of amino group of Phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para chlorination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para bromination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para florination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10573295 | 1999 | Enkephalin analog | 6 | Free | Free | Linear | L | Para iodination of amino group of phenylalanine | Derivative of Natural enkephalin | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | >300 | Mouse brain proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse brain proteases | in vitro | None | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 5.29 ±0.62 (t1/2 elimination) | Rat plasma proteases | Not mentioned | Intravenously administration to rat plasma | in vivo | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 0.62 ±0.05 (t1/2 elimination) | Rat plasma proteases | Not mentioned | Intravenously administration to rat plasma | in vivo | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 9.28 ±0.76 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 3.18 ±0.22 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10973845 | 2000 | Alpha 2-antiplasmin (α2AP ) | 24 | Free | Free | Linear | L | I125 radiolabeling | Human SERPINF2 gene | Clotting factor | 2 hours | 2 mg/ml | 19 | Mouse blood proteases | Not mentioned | Mouse blood fibrin clots | in vitro | None | None | Immunoblotting 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. | |||
| 10973845 | 2000 | Alpha 2-antiplasmin peptide (α2AP13-24 ) | 12 | Free | Free | Linear | L | Biotinylation at lysine residue(position 24) | Human SERPINF2 gene | Clotting factor | 2 hours | 0.5mMol/L | 21 | Mouse blood proteases | Not mentioned | Mouse blood fibrin clots | in vitro | None | None | Immunoblotting 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. | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 5.9 ±2.5 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Intravenous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 106 ±22 (t1/2 β) | New Zeland female rabbits blood protease | Radioimmunoassay | Intravenous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 1 μg/kg | 6.6 ±2.7 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 1 μg/kg | 112 ±41 (t1/2 β) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 5.3 ±1.1 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 103 ±19 (t1/2 β) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 100 μg/kg | 7.8 ±2.0 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 100 μg/kg | 173 ±13 (t1/2 β) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 3.2 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion 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. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.9 ±0.02 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion 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. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 2.8 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 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. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.6 ±0.5 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 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. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 203 ±10.2 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion 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. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 185.4 ±4.7 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion 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. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 111.1 ±3.9 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 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. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 140.2 ±2.5 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 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. | |||
| 10377427 | 1999 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 1.44 ±0.05 | Npr3+/+ mice blood proteases | Radioimmunoassay | Npr3+/+ mice blood sample | in vivo | 6230082 | None | Blood pressure=118.7 ±1.9 mmHg | |||
| 10377427 | 2000 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 2.4 ±0.08 | Npr3-/- mice blood proteases | Radioimmunoassay | Npr3-/- mice blood sample | in vivo | 6230082 | None | Blood pressure=110.4 ±2.3 mmHg | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg | 21.6 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg | 30.2 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg | 23 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg | 20.4 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg | 18.2 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg | 19.4 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 37 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 2μg/kg | 68 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 47 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 25μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 100μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 2μg/kg | 39 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 1 | 26.1 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 1 | 25.4 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 1 | 23.4 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 1 | 23.7 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 1 | 33.8 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 1 | 24.2 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 14 | 27.2 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 14 | 32.7 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 14 | 44 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 14 | 25.1 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 14 | 39.3 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet 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. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 14 | 31.3 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet 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. |