PZ0412
PF-06427878
≥98% (HPLC)
别名:
(R)-3-((2-(3-(2-Ethoxyphenoxy)piperidin-1-yl)pyrimidine-5-carboxamido)methyl)benzoic acid, 3-[[[[2-[(3R)-3-(2-Ethoxyphenoxy)-1-piperidinyl]-5-pyrimidinyl]carbonyl]amino]methylbenzoic acid, PF 06427878, PF06427878
产品名称
PF-06427878, ≥98% (HPLC)
InChI
1S/C26H28N4O5/c1-2-34-22-10-3-4-11-23(22)35-21-9-6-12-30(17-21)26-28-15-20(16-29-26)24(31)27-14-18-7-5-8-19(13-18)25(32)33/h3-5,7-8,10-11,13,15-16,21H,2,6,9,12,14,17H2,1H3,(H,27,31)(H,32,33)/t21-/m1/s1
InChI key
IDVOZBCJUVAIMF-OAQYLSRUSA-N
SMILES string
O=C(C1=CC=CC(CNC(C2=CN=C(N=C2)N3C[C@@H](CCC3)OC4=CC=CC=C4OCC)=O)=C1)O
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Quality Level
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.).
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Neeta B Amin et al.
Science translational medicine, 11(520) (2019-11-30)
Nonalcoholic steatohepatitis (NASH) is characterized by the accumulation of hepatocyte triglycerides, the synthesis of which is catalyzed by diacylglycerol acyltransferases (DGATs). Here, we investigate DGAT2 as a potential therapeutic target using an orally administered, selective DGAT2 inhibitor, PF-06427878. Treatment with
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