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编 号:F107505
分子式:C18H20Cl2N6O2
分子量:423.3
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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生物活性:
Ibezapolstat (ACX-362E) is a first-in-class, orally active DNA polymerase IIIC (pol IIIC) inhibitor, with a Ki of 0.325 μM for the DNA pol IIIC from C. difficile. Ibezapolstat is developed for the research of C. difficile infection(CDI).

体内研究:
Ibezapolstat is poorly absorbed and apparently nontoxic in the hamster C. difficile-associated disease (CDAD) model (potential for achieving a high local concentration at the site of C. difficile infection in the colon).Ibezapolstat (50 mg/kg; p.o.; twice daily; for 3 days) shows strong anti-C. difficile properties in the hamster CDAD model.Animal Model:Female golden Syrian hamsters (80-90 g), CDAD model
Dosage:50 mg/kg
Administration:Oral administration, twice daily, for 3 days
Result:Completely protected C. difficile-infected animals for a period of up to 5 days.

体外研究:
Ibezapolstat binds to and inhibits DNA pol IIIC from aerobic and low G+C Gram-positive bacteria.Ibezapolstat displays antibacterial activities against broad spectrum ofC. difficilepathogens, with an MIC range of 1-8 μg/mL for a panel of 104 clinical isolates ofC. difficile overall in vitro.
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