For research use only. Not for therapeutic Use.
Angiopeptin TFA, a cyclic octapeptide analogue of somatostatin, is a weak sst2/sst5 receptor partial agonist with IC50 values of 0.26 nM and 6.92 nM, respectively. Angiopeptin TFA is a potent inhibitor of growth hormone release and insulin-like growth factor-1 (IGF-1) production. Angiopeptin TFA inhibits adenylate cyclase or stimulates extracellular acidification. Angiopeptin TFA has the potential for coronary atherosclerosis research[1][2].
Angiopeptin (0.1 nM- 10 μM; for 1 h) TFA acts as a partial agonist (pEC50=6.57) with a maximum response of 423% at 3 μM on the release of tritium on CHO hsst2 cells[2].
Angiopeptin (20 and 50μg/kg; i.h.) TFA significantly inhibits neointimal formation[1].
Angiopeptin (20 μg/kg; per day) TFA significantly inhibits coronary artery myointimal proliferation in cardiac allografts by appmximalely 50%[1].
| Catalog Number | I044304 |
| CAS Number | 2478421-60-0 |
| Synonyms | (2S)-6-amino-N-[(2S)-1-[[(2R)-1-[[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-sulfanylpropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-2-[[(2R)-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-3-sulfanylpropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanamide;2,2,2-trifluoroacetic acid |
| Molecular Formula | C58H73F6N11O14S2 |
| Purity | ≥95% |
| InChI | InChI=1S/C54H71N11O10S2.2C2HF3O2/c1-29(2)45(54(75)63-44(28-77)53(74)65-46(30(3)66)47(57)68)64-49(70)40(14-8-9-21-55)59-51(72)42(25-35-26-58-39-13-7-6-12-37(35)39)61-50(71)41(24-31-16-19-36(67)20-17-31)60-52(73)43(27-76)62-48(69)38(56)23-32-15-18-33-10-4-5-11-34(33)22-32;2*3-2(4,5)1(6)7/h4-7,10-13,15-20,22,26,29-30,38,40-46,58,66-67,76-77H,8-9,14,21,23-25,27-28,55-56H2,1-3H3,(H2,57,68)(H,59,72)(H,60,73)(H,61,71)(H,62,69)(H,63,75)(H,64,70)(H,65,74);2*(H,6,7)/t30-,38-,40+,41+,42-,43+,44+,45+,46+;;/m1../s1 |
| InChIKey | PLVCOVWXYIMTNV-XCNZXRHRSA-N |
| SMILES | CC(C)C(C(=O)NC(CS)C(=O)NC(C(C)O)C(=O)N)NC(=O)C(CCCCN)NC(=O)C(CC1=CNC2=CC=CC=C21)NC(=O)C(CC3=CC=C(C=C3)O)NC(=O)C(CS)NC(=O)C(CC4=CC5=CC=CC=C5C=C4)N.C(=O)(C(F)(F)F)O.C(=O)(C(F)(F)F)O |
| Reference | [1]. Lundergan CF, et al. Peptide inhibition of myointimal proliferation by angiopeptin, a somatostatin analogue. J Am Coll Cardiol. 1991;17(6 Suppl B):132B-136B. [2]. Alderton F, et al. Somatostatin receptor-mediated arachidonic acid mobilization: evidence for partial agonism of synthetic peptides. Br J Pharmacol. 2001;132(3):760-766. |
