PF-06427878 (C005B-432392)

Biochem/physiol Actions

PF-06427878 is an orally active, potent and selective diacylglycerol acyltransferase 2 inhibitor (human/rat DGAT2 IC₅₀ = 99/202 nM; >470-fold selectivity over DGAT1, MGAT1/2/3) that inhibits DGAT2-dependent triglyceride (TG) synthesis in primary human hepatocytes (IC₅₀ = 11.6 nM in the presence of DGAT1 inhibitor PF-04620110). 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.). Likewise, 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.).

Legal Information

Sold for research purposes under agreement from Pfizer Inc.

UPC:

12352211

Condition:

New

Weight:

1.00 Ounces

HazmatClass:

No

Quantity:

25

Unit of Measurement:

MG

MPN:

PZ0412-25MG

CAS:

1809064-23-0