1469284-79-4
1469284-79-4 structure
- Name: PF 06424439
- Chemical Name: PF-06424439 methanesulfonate
- CAS Number: 1469284-79-4
- Molecular Formula: C23H30ClN7O4S
- Molecular Weight: 536.05
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Acyltransferase
- Create Date: 2019-08-03 21:51:58
- Modify Date: 2024-01-04 12:10:45
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PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate[2].
| Name | PF-06424439 methanesulfonate |
|---|
| Description | PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM[1]. PF-06424439 methanesulfonate 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 methanesulfonate (p.o.; 60 mg/kg/day; for 3 days) reduces plasma TG and cholesterol levels and decreases nonsignificant in circulating lipids in mice (Ldlr-/-)[1]. PF-06424439 methanesulfonate (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 | C23H30ClN7O4S |
|---|---|
| Molecular Weight | 536.05 |
| RIDADR | NONH for all modes of transport |
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