产品
编 号：F741891
分子式：C26H33N6O7P
分子量：572.55
分子式：C26H33N6O7P
分子量：572.55
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1001419-18-6
产品详情
生物活性：
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.
体内研究：
BMS-820132 (化合物 31) (3 μmol/kg，30 μmol/kg；口服；单剂量) 在口服葡萄糖耐量试验 (OGTT) 中降低高脂肪饮食诱导的肥胖 (DIO) 小鼠的葡萄糖水平。BMS-820132 (10-200 mg/kg；口服；每天一次，持续 1 个月) 导致正常大鼠体重下降，但对 ZDF 大鼠没有影响，这表明 BMS-820132 毒性是继发于强效 GK 激活的药理学作用[ 2]。BMS-820132 (10 mg/kg-120 mg/kg；口服；每天一次，持续 1 个月) 对狗的食物消耗没有显着影响。在动物模型中的药代动力学分析RouteDose (mg/kg)Cmax (μM)Tmax (h)AUC0-24 h (μM·h)T1/2 (h)CLTp (mL/min/kg)Vss (L/kg)F (L/kg)
mouseiv2.524.92.12.90.3
po514.10.549.7100
rativ2.516.60.94.40.3
po513.00.929.590
dogiv312.31.87.20.5
po34.90.88.066
monkeyiv33.81.922.71.1
po33.81.30.5715
Animal Model:Zucker diabetic fatty (ZDF) rats and normal SD rats
Dosage:10 mg/kg, 50 mg/kg, 200 mg/kg
Administration:PO; once daily for 1 month
Result:Resulted reductions in body weight gains starting on day 7 in SD rats (11% lower than controls), but not ZDF rats.
Animal Model:Beagle dogs
Dosage:10 mg/kg, 60 mg/kg, 120 mg/kg
Administration:PO; once daily for 1 month
Result:There were no meaningful differences in food consumption in dogs model.
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation.
体内研究：
BMS-820132 (化合物 31) (3 μmol/kg，30 μmol/kg；口服；单剂量) 在口服葡萄糖耐量试验 (OGTT) 中降低高脂肪饮食诱导的肥胖 (DIO) 小鼠的葡萄糖水平。BMS-820132 (10-200 mg/kg；口服；每天一次，持续 1 个月) 导致正常大鼠体重下降，但对 ZDF 大鼠没有影响，这表明 BMS-820132 毒性是继发于强效 GK 激活的药理学作用[ 2]。BMS-820132 (10 mg/kg-120 mg/kg；口服；每天一次，持续 1 个月) 对狗的食物消耗没有显着影响。在动物模型中的药代动力学分析RouteDose (mg/kg)Cmax (μM)Tmax (h)AUC0-24 h (μM·h)T1/2 (h)CLTp (mL/min/kg)Vss (L/kg)F (L/kg)
mouseiv2.524.92.12.90.3
po514.10.549.7100
rativ2.516.60.94.40.3
po513.00.929.590
dogiv312.31.87.20.5
po34.90.88.066
monkeyiv33.81.922.71.1
po33.81.30.5715
Animal Model:Zucker diabetic fatty (ZDF) rats and normal SD rats
Dosage:10 mg/kg, 50 mg/kg, 200 mg/kg
Administration:PO; once daily for 1 month
Result:Resulted reductions in body weight gains starting on day 7 in SD rats (11% lower than controls), but not ZDF rats.
Animal Model:Beagle dogs
Dosage:10 mg/kg, 60 mg/kg, 120 mg/kg
Administration:PO; once daily for 1 month
Result:There were no meaningful differences in food consumption in dogs model.
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