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Catalog Number:
E1KS2674 Amount:
5mg1 PHYSICAL AND CHEMICAL PROPERTIES
2 Biological Activity
A 922500 is a potent and selective diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50 of 7 and 22nM for human and mouse DGAT-1, respectively.
Diacylglycerol acyltransferases (DGAT) exert their action in the final reaction step in the synthesis of triglyceride. It was reported that DGAT-1 contributed to the development of diet-induced obesity (DIO) or insulin resistance. A 922500 has less inhibitory activity against DGAT-2, phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 than DGAT-1. A 922500 inhibited DGAT-2, phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 53 and 296μM, respectively. A 922500 doesn’t affect food intake. Meanwhile, A 922500 reduces triglyceride levels of liver and plasma in vivo. [1][2]
3 References:
http://www.ncbi.nlm.nih.gov/pubmed/19478132 King AJ et al. J Pharmacol Exp Ther. 2009 Aug;330(2):526-31.
http://www.ncbi.nlm.nih.gov/pubmed/20805092 Qi J et al. J Lipid Res. 2010 Dec;51(12):3559-67.
The pharmacological and toxicological properties of this product have not been fully investigated. Exercise caution in use and handling. This product must not be used in humans.