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PF-06427878 is a potent, selective, oral DGAT2 inhibitor with IC50 of 99/202 nM for human/rat DGAT2, >470-fold selectivity over DGAT1 and MGAT1/2/3.PF-06427878 inhibits DGAT2-dependent triglyceride (TG) synthesis in primary human hepatocytes with IC50 of 11.6 nM.PF-06427878 reduces hepatic and circulating plasma TG levels as well as lipogenic gene expression in rats maintained on a Western-type diet (0.3-30 mg/kg bid. po.).PF-06427878 significantly improves steatosis and hepatocellular ballooning with a decrease in lobular inflammation in a murine nonalcoholic steatohepatitis (NASH) model (2 or 20 mg/kg bid. po.).
TP-020 is a potent, selective, orally active inhibitor of monoacylglycerol acyltransferase (MGAT2) with IC50 of 7.8 and 2.4 nM for human and mouse MGAT2, respectively.
PF-06427878 is a potent, selective, oral DGAT2 inhibitor with IC50 of 99/202 nM for human/rat DGAT2, >470-fold selectivity over DGAT1 and MGAT1/2/3.PF-06427878 inhibits DGAT2-dependent triglyceride (TG) synthesis in primary human hepatocytes with IC50 of 11.6 nM.PF-06427878 reduces hepatic and circulating plasma TG levels as well as lipogenic gene expression in rats maintained on a Western-type diet (0.3-30 mg/kg bid. po.).PF-06427878 significantly improves steatosis and hepatocellular ballooning with a decrease in lobular inflammation in a murine nonalcoholic steatohepatitis (NASH) model (2 or 20 mg/kg bid. po.).
GSK2973980A is a potent and selective DGAT1 inhibitor with IC50 of 3 nM, exhibits >2,900-fold selectivity over human DGAT2, ACAT1 and ACAT2 (IC50>10 uM).
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