Pricing updated 2019-07-23. Prices are subject to change without notice.
T-863 is a potent inhibitor of diacylglycerol acetyltransferase-1 (DGAT-1; IC50 = 15 nM).1 It is selective for DGAT-1 over DGAT-2 and acyl-coenzyme A:cholesterol acyltransferase-1 (ACAT-1; IC50s = >10 and 12 μM, respectively). T-863 inhibits triacylglycerol synthesis in HuTu 80 cells (IC50 = 4 nM). In vivo, T-863 (20 mg/kg) reduces plasma triacylglycerol levels, the ratio of triacylglycerols to diacylglycerols, and body weight in a mouse model of diet-induced obesity.
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Birch, A.M., Birtles, S., Buckett, L.K., et al. Discovery of a potent, selective, and orally efficacious pyrimidinooxazinyl bicyclooctaneacetic acid diacylglycerol acyltransferase-