1469284-78-3
1469284-78-3 structure
- Name: PF-06424439
- Chemical Name: PF-06424439
- CAS Number: 1469284-78-3
- Molecular Formula: C22H26ClN7O
- Molecular Weight: 439.94
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
- Create Date: 2019-08-04 11:52:58
- Modify Date: 2024-01-08 10:48:50
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PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
| Name | PF-06424439 |
|---|
| Description | PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2]. |
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| Related Catalog | |
| Target |
IC50: 14 nM (DGAT2)[1] |
| In Vivo | PF-06424439 (p.o.; 60 mg/kg/day; for 3 days) reduces plasma triglyceride (TG) and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1]. PF-06424439 (i.v.; 1 mg/kg) shows moderate clearance in rats following intravenous administration and moderate steady-state volume of distribution (Vdss) results in a short half-life[1]. Animal Model: Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)[1] Dosage: 60 mg/kg Administration: P.o.; daily; for 3 days Result: Reduced plasma TG and cholesterol levels and decreased nonsignificant in circulating lipids. Animal Model: Male Wistar-Han rats[1] Dosage: 1 mg/kg Administration: I.v. Result: Showed moderate clearance and a short half-life with t1/2=1.39 h. |
| References |
| Molecular Formula | C22H26ClN7O |
|---|---|
| Molecular Weight | 439.94 |