产品
编 号：F014151
分子式：C20H22N4O2
分子量：350.41
分子式：C20H22N4O2
分子量：350.41
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1031336-60-3
产品详情
生物活性：
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
体内研究：
ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice.ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion indiet-induced obesity mice.Animal Model:Male CD-1 mice, postprandial hyperlipidemia model
Dosage:0.03, 0.3, or 3 mg/kg
Administration:Oral gavage, single dose
Result:Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).
Animal Model:Male C57BL/6J diet-induced obesity (DIO) mice
Dosage:0.3 mg/kg
Administration:Oral gavage, single dose
Result:Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.
Animal Model:CD-1 mice and Sprague-Dawley rats
Dosage:10 mg/kg or 5 mg/kg
Administration:Intravenous injection or oral gavage (Pharmacokinetic Analysis)
Result:Selected Pharmacokinetic Properties of ABT-046amouse (10 mg/kg) rat (5 mg/kg)
ivb
T1/2 (h)4.63.8
Vss (L/kg)0.30.3
Clp (L/h/kg)0.10.05
pob
T1/2 (h)5.15.6
Cmax (μg/mL)17.49.3
AUC (μg h/mL)151130
F (%)7891
a All values are mean values ± SEMs (n = 3 unless specified otherwise). b 1% Tween-80 in water.
体外研究：
ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 of 78 nM.ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively).ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers.
ABT-046 is a potent, selective, and orally active acyl CoA:diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of both 8 nM against human and mouse DGAT-1.
体内研究：
ABT-046 (0.03-3 mg/kg; i.g.; once) significantly reduced postprandial triglycerides in CD-1 mice.ABT-046 (0.3 mg/kg; i.g.; once) abolishes the postprandial triglyceride excursion indiet-induced obesity mice.Animal Model:Male CD-1 mice, postprandial hyperlipidemia model
Dosage:0.03, 0.3, or 3 mg/kg
Administration:Oral gavage, single dose
Result:Showed a dose-dependent reduction in serum triglycerides starting at 0.03 mg/kg and increasing through the higher doses (40, 60, and 90% reduction from vehicle at 0.03, 0.3, and 3.0 mg/kg, respectively). The ascending pharmacodynamics correlated well with a linear increase in plasma exposure going from 0.03 to 3 mg/kg (C2h = 0.033, 0.36, and 3.10 μg/mL at 0.03, 0.3, and 3.0 mg/kg, respectively).
Animal Model:Male C57BL/6J diet-induced obesity (DIO) mice
Dosage:0.3 mg/kg
Administration:Oral gavage, single dose
Result:Afforded a sustained reduction in serum triglyceride concentrations throughout the experiment.
Animal Model:CD-1 mice and Sprague-Dawley rats
Dosage:10 mg/kg or 5 mg/kg
Administration:Intravenous injection or oral gavage (Pharmacokinetic Analysis)
Result:Selected Pharmacokinetic Properties of ABT-046amouse (10 mg/kg) rat (5 mg/kg)
ivb
T1/2 (h)4.63.8
Vss (L/kg)0.30.3
Clp (L/h/kg)0.10.05
pob
T1/2 (h)5.15.6
Cmax (μg/mL)17.49.3
AUC (μg h/mL)151130
F (%)7891
a All values are mean values ± SEMs (n = 3 unless specified otherwise). b 1% Tween-80 in water.
体外研究：
ABT-046 shows no inhibition against human DGAT-2 and inhibits triglyceride formation in HeLa cells expressing human DGAT-1 with an IC50 of 78 nM.ABT-046 exhibits high in vitro permeability values in Caco-2 cells with no evidence of active efflux (efflux ratio = 1.4 and 1.1 at 0.5 and 5 μM, respectively).ABT-046 demonstrates negligible turnover in microsome preparations from mouse and human livers.
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