Potent and selective diacylglycerol acyltransferase (DGAT-1) inhibitor (IC50
= 0.6 nM). Exhibits selectivity for DGAT-1 over DGAT-2, Kv
11.1 (hERG) and cytochrome P450 enzymes. Suppresses triacylglyceride (TAG) plasma excursion and adipose tissue TAG synthesis in rats. Reduces body weight of diet-induced obese rats. Cell permeable and orally bioavailable.
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Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
McCoull et al.