A 922500

Cat. No. 3587

A 922500 C26H24N2O4 [959122-11-3]

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Alternative Name: DGAT-1 Inhibitor 4a

Chemical Name: (1R,2R)-2-[[4'-[[Phenylamino)carbonyl]amino] [1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid

Biological Activity

Diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo. Orally active.

Technical Data

Soluble to 50 mM in DMSO
>98 %
Desiccate at +4°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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King et al (2010) In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia. Eur.J.Pharmacol. 637 155. PMID: 20385122.

King et al (2009) Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the zucker fatty rat and the hyperlipidemic hamster. J.Pharmacol.Exp.Ther. 330 526. PMID: 19478132.

Zhao et al (2008) Validation of diacyl glycerolacyltransferase I as a novel target of obesity and dyslipidemia using a potent and selective small molecule inhibitor. J.Med.Chem. 51 380. PMID: 18183944.

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Citations are publications that use Tocris products. Selected citations for A 922500 include:

Velliquette et al (2015) Identification of a botanical inhibitor of intestinal diacylglyceride acyltransferase 1 activity via in vitro screening and a parallel, randomized, blinded, placebo-controlled clinical trial. Cell Rep 12 27. PMID: 26246845.

Camus et al (2013) Diacylglycerol acyltransferase-1 localizes hepatitis C virus NS5A protein to lipid droplets and enhances NS5A interaction with the viral capsid core. Nutr Metab (Lond) 288 9915. PMID: 23420847.

Poliakov et al (2012) Origin and evolution of retinoid isomerization machinery in vertebrate visual cycle: hint from jawless vertebrates. PLoS One 7 e49975. PMID: 23209628.

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Keywords: A 922500, supplier, Diacylglycerol, acyltransferase, 1, DGAT-1, inhibitors, inhibits, Transferases, A922500, Tocris Bioscience, Diacylglycerol O-Acyltransferase Inhibitor products

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