产品
编 号：F235611
分子式：C21H20ClF3N2O4
分子量：456.84
分子式：C21H20ClF3N2O4
分子量：456.84
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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结构图
CAS No: 1883747-71-4
产品详情
生物活性：
Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacterium tuberculosis.
体内研究：
Quabodepistat (OPC-167832) (口服给药；0.625-10 mg/kg) 具有良好的药代动力学特征。血浆在 0.5 h 至 1.0 h (tmax) 达到峰值，并以 1.3 h 至 2.1 h 的半衰期 (t1/2) 消除 Quabodepistat 在肺中的浓度约为血浆中的 2 倍，Quabodepistat 在血浆和肺中的 Cmax 和 AUCt 呈剂量依赖性。与载体组相比，Quabodepistat (口服；0.625-10 mg/kg；4 周) 显著降低肺 CFU。从 0.625 mg/kg 到 2.5 mg/kg 观察到肺 CFU 的剂量依赖性降低。在 M.Kurono 感染的 ICR 雌性小鼠模型。Quabodepistat 通过口服灌胃与 DMD、BDQ 或 LVX 联合使用时，其疗效显著高于单独使用每种药物。与 DC、DCB 相比，Quabodepistat (口服灌胃；2.5 mg/kg；与 DCMB 联合使用；12 周) 显示出最有效的疗效。处理 6 周后的肺部 CFU 计数低于检测限，而在仅仅 8 周的处理结束时，所有被评估小鼠的肺部细菌都已被根除。Animal Model:ICR mice
Dosage:0.625-10 mg/kg
Administration:Oral administration; 0.625-10 mg/kg; 4?weeks
Result:Exhibited in vivo?efficacy against a mouse chronic TB model.
体外研究：
Quabodepistat (OPC-167832) exhibits very low MICs against laboratory strains of?M. tuberculosis?H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, Quabodepistat has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria.The IC90 values of Quabodepistat against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027?μg/ml, respectively. Quabodepistat shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004?μg/ml or higher.
Quabodepistat (OPC-167832) is a potent and orally active dprE1 inhibitor with?an IC50 of 0.258 μM. Quabodepistat has antituberculosis activity and can be used for the research of tuberculosis?caused by?Mycobacterium tuberculosis.
体内研究：
Quabodepistat (OPC-167832) (口服给药；0.625-10 mg/kg) 具有良好的药代动力学特征。血浆在 0.5 h 至 1.0 h (tmax) 达到峰值，并以 1.3 h 至 2.1 h 的半衰期 (t1/2) 消除 Quabodepistat 在肺中的浓度约为血浆中的 2 倍，Quabodepistat 在血浆和肺中的 Cmax 和 AUCt 呈剂量依赖性。与载体组相比，Quabodepistat (口服；0.625-10 mg/kg；4 周) 显著降低肺 CFU。从 0.625 mg/kg 到 2.5 mg/kg 观察到肺 CFU 的剂量依赖性降低。在 M.Kurono 感染的 ICR 雌性小鼠模型。Quabodepistat 通过口服灌胃与 DMD、BDQ 或 LVX 联合使用时，其疗效显著高于单独使用每种药物。与 DC、DCB 相比，Quabodepistat (口服灌胃；2.5 mg/kg；与 DCMB 联合使用；12 周) 显示出最有效的疗效。处理 6 周后的肺部 CFU 计数低于检测限，而在仅仅 8 周的处理结束时，所有被评估小鼠的肺部细菌都已被根除。Animal Model:ICR mice
Dosage:0.625-10 mg/kg
Administration:Oral administration; 0.625-10 mg/kg; 4?weeks
Result:Exhibited in vivo?efficacy against a mouse chronic TB model.
体外研究：
Quabodepistat (OPC-167832) exhibits very low MICs against laboratory strains of?M. tuberculosis?H37Rv (MIC: 0.0005 μg/ml) and Kurono (MIC: 0.0005 μg/ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg/ml). However, Quabodepistat has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria.The IC90 values of Quabodepistat against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027?μg/ml, respectively. Quabodepistat shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004?μg/ml or higher.
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