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CAS No. : 1883747-71-4
MCE 国际站:Quabodepistat
产品活性:Quabodepistat (OPC-167832) 是一种有效的口服活性 dprE1 抑制剂,其>IC50 为 0.258 μM。Quabodepistat 具有抗结核活性,可用于由结核分枝杆菌引起的结核病的相关研究。
研究领域:Anti-infection
作用靶点:Bacterial
In Vitro: 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.
In Vivo: Quabodepistat (OPC-167832) (oral administration; 0.625-10 mg/kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1/2) of 1.3 h to 2.1 h Quabodepistat distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of Quabodepistat in plasma and the lungs shows dose dependency.Quabodepistat (oral administration; 0.625-10 mg/kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg/kg to 2.5 mg/kg. In a M. tuberculosis Kurono-infected ICR female mice model. Quabodepistat combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone..Quabodepistat (oral gavage; 2.5 mg/kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate.
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