A 922500

• CAT Number: I005686
• CAS Number: 959122-11-3
• Molecular Formula: C26H24N2O4
• Molecular Weight: 428.5
• Purity: ≥95%
• Target: Transferase
• Solubility: DMSO 86 mg/ml; Water < 1 mg/ml
• Storage: Desiccate at +4°C
• IC50: 7 nM(human DGAT-1); 24 nM(DGAT-1)
• InChI: InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
• InChIKey: BOZRFEQDOFSZBV-DHIUTWEWSA-N
• SMILES: O=C(NC1=CC=C(C2=CC=C(C([C@@H]3CCC[C@H]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4

A 922500 (CAT: I005686) is a potent and selective inhibitor of diacylglycerol O-acyltransferase 1 (DGAT-1). DGAT-1 is an enzyme involved in the synthesis of triglycerides, which play a critical role in lipid metabolism. By inhibiting DGAT-1, A 922500 effectively reduces the formation of triglycerides. It exhibits high potency with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1, respectively. The selective inhibition of DGAT-1 by A 922500 makes it a potential therapeutic agent for the treatment of metabolic disorders, such as obesity and non-alcoholic fatty liver disease.

Reference

[1]. Zhao, Gang; Souers, Andrew J.; Validation of Diacyl Glycerolacyltransferase I as a Novel Target for the Treatment of Obesity and Dyslipidemia Using a Potent and Selective Small Molecule Inhibitor . Journal of Medicinal Chemistry (2008), 51(3), 380-383. 


[2]. King, Andrew J.; Segreti, Jason A.; Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster. Journal of Pharmacology and Experimental Therapeutics (2009), 330(2), 526-531. 


[3]. King AJ, Segreti JA, Larson KJ, Souers AJ, Kym PR, Reilly RM, Collins CA, Voorbach MJ, Zhao G, Mittelstadt SW, Cox BF.In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia.Eur J Pharmacol. 2010 Jul 10;637(1-3):155-61. Epub 2010 Apr 10.