产品
编 号：F399401
分子式：C30H36ClN3O3
分子量：522.08
分子式：C30H36ClN3O3
分子量：522.08
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
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: 591778-70-0
产品详情
生物活性：
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.
体内研究：
CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy.CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses.CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level.Animal Model:Male ob/ob mice
Dosage:4.6-21 mg/kg
Administration:Oral gavage; 4.6-21 mg/kg; once
Result:Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment.
Animal Model:Male Sprague-Dawley rats
Dosage:Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg
Administration:Intravenous injection and oral gavage; intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once
Result:Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ of 960 ng?h/mL.
Animal Model:Male ob/ob mice
Dosage:Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg
Administration:Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once
Result:Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ of 3068 ng?h/mL.
Animal Model:Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Resulted in time-dependent reductions in RQ (a ratio of CO2 production to O2 consumption) of up to 64%.
体外研究：
CP-640186 (20 μM; 48 h) treatment can inhibit H460 cell growth.CP-640186 (0.1 nM-100 μM; 2 h) treatment increases fatty acid metabolism in a concentration-dependent manner in C2C12 cells and muscle strips.CP-640186 (0.62-1.8 μM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells.
CP-640186 hydrochloride is an orally active and cell-permeable Acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 53 nM and 61 nM for rat liver ACC1 and rat skeletal muscle ACC2 respectively. Acetyl-CoA carboxylase (ACC) is a key enzyme of fatty acid metabolism that enables the synthesis of malonyl-CoA. CP-640186 hydrochloride can also stimulate muscle fatty acid oxidation.
体内研究：
CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy.CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses.CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level.Animal Model:Male ob/ob mice
Dosage:4.6-21 mg/kg
Administration:Oral gavage; 4.6-21 mg/kg; once
Result:Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment.
Animal Model:Male Sprague-Dawley rats
Dosage:Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg
Administration:Intravenous injection and oral gavage; intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once
Result:Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ of 960 ng?h/mL.
Animal Model:Male ob/ob mice
Dosage:Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg
Administration:Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once
Result:Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ of 3068 ng?h/mL.
Animal Model:Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Resulted in time-dependent reductions in RQ (a ratio of CO2 production to O2 consumption) of up to 64%.
体外研究：
CP-640186 (20 μM; 48 h) treatment can inhibit H460 cell growth.CP-640186 (0.1 nM-100 μM; 2 h) treatment increases fatty acid metabolism in a concentration-dependent manner in C2C12 cells and muscle strips.CP-640186 (0.62-1.8 μM; 2 h) treatment inhibits fatty acid synthesis and TG synthesis in HepG2 cells.
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