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Description: PF-04620110 (PF04620110; PF 04620110) is a novel, potent, orally bioactive, and selective diglyceride acyltransferase-1 (DGAT1) inhibitor with the potential to treat type 2 diabetes mellitus. It inhibits DGAT1 with an IC50 of 19 nM. PF-04620110 has been advanced to clinical trials on the basis of the excellent pharmacologic and pharmacokinetic profiles. F-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of >=0.1 mg/kg following a lipid challenge.
References: ACS Med Chem Lett. 2011; 2(5):407-12; Am J Physiol Gastrointest Liver Physiol. 2013; 304(11):G958-69.
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