For research use only. Not for therapeutic Use.
Allo-aca, a leptin peptidomimetic, is a potent, specific leptin receptor antagonist peptide. Allo-aca blocks leptin signaling and action in numerous in vitro and in vivo models[1][2].
Allo-aca inhibits leptin-induced proliferation of MDA-MB-231 cells at 50 pM concentration. Allo-aca inhibits leptin-induced proliferation of MCF-7 cells with an IC50 of 200 pM[1].
Allo-aca at 250 nmol/L reduces VEGF-dependent leptin mRNA expression in both cell lines below base levels. Allo-aca inhibits VEGF mitogenic effects. Allo-aca inhibits VEGF-induced chemotaxis and chemokinesis in RF/6A retinal endothelial cells[2].
In an MDA-MB-231 orthotopic mouse xenograft model, Allo-aca administered subcutaneously significantly extends the average survival time from 15.4 days (untreated controls) to 24 and 28.1 days at 0.1 and 1mg/kg/day doses, respectively[1].
| Catalog Number | I044196 |
| Synonyms | (4S)-4-[[(2S,3S)-2-amino-3-hydroxybutanoyl]amino]-5-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[4-(2-amino-2-oxoethyl)-2-oxochromen-7-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]amino]-5-oxopentanoic acid |
| Molecular Formula | C48H75N13O15 |
| Purity | ≥95% |
| InChI | InChI=1S/C48H75N13O15/c1-8-10-29(56-42(70)31(14-15-36(65)66)58-46(74)38(50)25(7)63)43(71)61-39(23(4)5)47(75)54-24(6)40(68)59-32(17-22(2)3)44(72)60-33(21-62)45(73)57-30(11-9-16-53-48(51)52)41(69)55-27-12-13-28-26(18-35(49)64)19-37(67)76-34(28)20-27/h12-13,19-20,22-25,29-33,38-39,62-63H,8-11,14-18,21,50H2,1-7H3,(H2,49,64)(H,54,75)(H,55,69)(H,56,70)(H,57,73)(H,58,74)(H,59,68)(H,60,72)(H,61,71)(H,65,66)(H4,51,52,53)/t24-,25-,29-,30-,31-,32-,33-,38-,39-/m0/s1 |
| InChIKey | HBIZXCPYXWQUEB-PPHQEZGGSA-N |
| SMILES | CCCC(C(=O)NC(C(C)C)C(=O)NC(C)C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)NC(CCCN=C(N)N)C(=O)NC1=CC2=C(C=C1)C(=CC(=O)O2)CC(=O)N)NC(=O)C(CCC(=O)O)NC(=O)C(C(C)O)N |
| Reference | [1]. Otvos L Jr, et al. Efficacy of a leptin receptor antagonist peptide in a mouse model of triple-negative breast cancer. Eur J Cancer. 2011;47(10):1578-1584. [2]. Coroniti R, et al. Designer Leptin Receptor Antagonist Allo-aca Inhibits VEGF Effects in Ophthalmic Neoangiogenesis Models [published correction appears in Front Mol Biosci. 2016 Nov 18;3:75]. Front Mol Biosci. 2016;3:67. Published 2016 Oct 13. |
