PZ0412

PF-06427878

≥98% (HPLC)

• Synonym(e): (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
• Empirische Formel (Hill-System): C₂₆H₂₈N₄O₅
• CAS-Nummer: 1809064-23-0
• Molekulargewicht: 476.52
• UNSPSC-Code: 51111800
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: room temp
• SMILES String: O=C(C1=CC=CC(CNC(C2=CN=C(N=C2)N3C[C@@H](CCC3)OC4=CC=CC=C4OCC)=O)=C1)O
• 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
• InChIKey: IDVOZBCJUVAIMF-OAQYLSRUSA-N

Beschreibung

Biochem./physiol. Wirkung

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.).

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable