产品
编 号:F504544
分子式:C23H22F2N4O4
分子量:456.44
产品类型
结构图
CAS No: 892489-52-0
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产品详情
生物活性:
AZD3988 is an orally active diacylglycerol acyl transferase-1 (DGAT-1) inhibitor. AZD3988 has excellent DGAT-1 (human) potency with an IC50 value of 0. 6 nM. AZD3988 can be used for the research of metabolic diseases such as diabetes, obesity.
体内研究:
AZD3988 (compound 53) shows (i.v., p.o.; 0.5, 1, 2, 5 mg/kg) has good pharmacokinetics in vivo efficacy.Animal Model:Mouse, Rats and Dog
Dosage:0.5, 1, 2, 5 mg/kg
Administration:IV at 0.5 mg/kg (mouse), 2 mg/kg (rat) and 1 mg/kg (dog) and po at 1 mg/kg (mouse), 5 mg/kg(rat) and 1 mg/kg (dog)
Result:Species Clp (mL/min/kg) Vdss(L/kg)IV half-life (h)po half-life (h) po Cmax(lM) Bioavailability (%)
Mouse4.60.994.94.71.9>100
Rat1.10.353.45.820>100
Dog2.50.361.85.71.532
体外研究:
AZD3988 (compound 53) (10 μM) can inhibit DGAT-1 with IC50 values of0. 6 nM (human), 0. 5nM (rat), 1.1 nM (mouse) and 0.5 nM (HuTu 80 cell), respectively.