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Chemical Structure : PF-06427878
Catalog No.: PC-73119Not For Human Use, Lab Use Only.
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.
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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.).
| M.Wt | 476.533 | |
| Formula | C26H28N4O5 | |
| Appearance | Solid | |
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1. Amin NB, et al. Sci Transl Med. 2019 Nov 27;11(520). pii: eaav9701. doi: 10.1126/scitranslmed.aav9701.
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