A 922500 is a diacyl glycerolacyltransferase 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.
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. 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.
Soluble in DMSO (50 mM), ethanol (~0.2 mg/ml), DMF (~20 mg/ml), DMSO:PBS (1:10 pH 7.2) (~0.1 mg/ml), and water (<1 mg/ml) at 25° C.
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Rated 5 out of
Tsuda et alTsuda et al. (PubMed ID 25405858) found that A- 922500 attenuated obesity and insulin resistance without causing skin problems in mice via DGAT1 inhibition. -SCBT Publication Review
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