Chemical Name: (1R,2R)-2-[[4'-[[Phenylamino)carbonyl]amino] [1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid
Biological ActivityA 922500 is a 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
In vivo efficacy of acyl CoA: diacylglycerol acyltransferase (DGAT) 1 inhibition in rodent models of postprandial hyperlipidemia.
King et al.
Validation of diacyl glycerolacyltransferase I as a novel target of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Zhao et al.
Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the zucker fatty rat and the hyperlipidemic hamster.
King et al.
Citations for A 922500
The citations listed below are publications that use Tocris products. Selected citations for A 922500 include:
4 Citations: Showing 1 - 4
TFAP2 transcription factors are regulators of lipid droplet biogenesis.
Authors: Scott Et al.
Identification of a botanical inhibitor of intestinal diacylglyceride acyltransferase 1 activity via in vitro screening and a parallel, randomized, blinded, placebo-controlled clinical trial.
Authors: Velliquette Et al.
Cell Rep 2015;12:27
Diacylglycerol acyltransferase-1 localizes hepatitis C virus NS5A protein to lipid droplets and enhances NS5A interaction with the viral capsid core.
Authors: Camus Et al.
Nutr Metab (Lond) 2013;288:9915
Origin and evolution of retinoid isomerization machinery in vertebrate visual cycle: hint from jawless vertebrates.
Authors: Poliakov Et al.
PLoS One 2012;7:e49975
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