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.

Product information

Molecular Weight: 1074.19

Formula: C48H75N13O15

Chemical Name: (6S, 9S, 12S, 15S, 18S, 21S, 24S)-1-amino-6-((4-(2-amino-2-oxoethyl)-2-oxo-2H-chromen-7-yl)carbamoyl)-24-((2S, 3R)-2-amino-3-hydroxybutanamido)-9-(hydroxymethyl)-1-imino-12-isobutyl-18-isopropyl-15-methyl-8, 11, 14, 17, 20, 23-hexaoxo-21-propyl-2, 7, 10, 13, 16, 19, 22-heptaazaheptacosan-27-oic acid

Smiles: CCC[C@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](N)[C@@H](C)O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NC1=CC2OC(=O)C=C(CC(N)=O)C=2C=C1

InChiKey: HBIZXCPYXWQUEB-JPBZROOYSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. 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.

In Vivo:

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.

Products are for research use only. Not for human use.