PF-04620110

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-04620110 是一种有效的、选择性的、口服生物可利用的 DGAT-1 抑制剂，IC50 为 19 nM，对 DGAT-2 没有活性（IC50>30 uM）。

PF-04620110 is a potent, selective, orally bioavailable DGAT-1 inhibitor with IC50 of 19 nM, shows no acitivity for DGAT-2 (IC50>30 uM); shows high selectivity versus a broad panel of off-target pharmacologic end points; inhibits triglyceride synthesis of 3 in the intestinal-derived HT-29 cell line with IC50 of 8 nM; demonstrates in vivo DGAT-1 inhibitionthrough reduction of plasma triglyceride levels in rodent, alters the temporal and spatial pattern of dietary lipid absorption in vivo.Diabetes Phase 1 Discontinued.

PF-04620110 is orally bioavailable, has passive permeability(1x10-6 cm/s).PF-04620110 inhibits DGAT-1 with an IC50 of 19 nM, and inhibits triglyceride synthesis with an IC50 of 8 nM in HT-29 cells.PF-04620110 is a highly selective inhibitor of DGAT-1 with >100-fold selectivity against a panel of lipid processing enzymes (human DGAT-2, several human acyl-CoA: cholesterol acyltransferase-1, wax alcohol acyltransferase-1/-2 and monacylglycerol acyltransferase-2/-3, and mouse MGAT-1).

PF-04620110 (0.1-10 mg/kg; p.o.) reduces plasma triglyceride levels at doses of ≥0.1 mg/kg following a lipid challenge in rat. Animal Model:Sprague?Dawley rats Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg Administration:Oral administration Result:Produced a statistically significant reduction in plasma triglyceride excursion at 2 hours to near prelipid load levels.

PF 04620110 | PF04620110

Metabolic Enzyme/Protease

DGAT

DGAT1

Metabolic Disease

Diabetes

1109276-89-2

396.4397

C21H24N4O4

>98% (HPLC)

10 mM in DMSO

C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)N3CCOC4=NC=NC(=C4C3=O)N

Cyclohexaneacetic acid, 4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-, trans-

(-20℃)

With Ice Pack

≥ 2 years