产品
编 号：F170735
分子式：C23H30ClN7O4S
分子量：536.05
分子式：C23H30ClN7O4S
分子量：536.05
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1469284-79-4
产品详情
生物活性：
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
体内研究：
PF-06424439 methanesulfonate (口服；60 mg/kg/天；持续 3 天) 降低小鼠血浆 TG 和胆固醇水平，并降低循环脂质 (Ldlr-/-)。 PF-06424439 methanesulfonate (静脉注射；1 mg/kg) 在大鼠静脉内给药后表现出中等清除率，中等稳态分布容积 (Vdss)，半衰期短。Animal Model:Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
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
Dosage:1 mg/kg
Administration:I.v.
Result:Showed moderate clearance and a short half-life with t1/2=1.39 h.
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate.
体内研究：
PF-06424439 methanesulfonate (口服；60 mg/kg/天；持续 3 天) 降低小鼠血浆 TG 和胆固醇水平，并降低循环脂质 (Ldlr-/-)。 PF-06424439 methanesulfonate (静脉注射；1 mg/kg) 在大鼠静脉内给药后表现出中等清除率，中等稳态分布容积 (Vdss)，半衰期短。Animal Model:Male low-density lipoprotein receptor (Ldlr) knockout mice (Ldlr-/-)
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
Dosage:1 mg/kg
Administration:I.v.
Result:Showed moderate clearance and a short half-life with t1/2=1.39 h.
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