| Identification | Back Directory | [Name]
2(1H)-Quinolinone, 5-[[(3R,4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxy-4-piperidinyl]methoxy]-8-fluoro-3,4-dihydro- | [CAS]
1883747-71-4 | [Synonyms]
OPC-167832
OPC167832,OPC 167832
Quabodepistat（OPC-167832）
2(1H)-Quinolinone, 5-[[(3R,4R)-1-(4-chloro-2,6-difluorophenyl)-3,4-dihydroxy-4-piperidinyl]methoxy]-8-fluoro-3,4-dihydro- | [Molecular Formula]
C21H20ClF3N2O4 | [MDL Number]
MFCD34473230 | [MOL File]
1883747-71-4.mol | [Molecular Weight]
456.84 |
| Chemical Properties | Back Directory | [Boiling point ]
645.6±55.0 °C(Predicted) | [density ]
1.485±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 180 mg/mL (394.01 mM; Need ultrasonic) | [form ]
Solid | [pka]
13.08±0.40(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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[1].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[1].[1].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[1]. | Animal Model: | ICR mice[1] | | 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. |
| [References]
[1] Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19. DOI:10.1128/AAC.02020-19 |
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