Description
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).
Product information
CAS Number: 1275582-97-2
Molecular Weight: 423.30
Formula: C18H20Cl2N6O2
Chemical Name: 2-{[(3,4-dichlorophenyl)methyl]amino}-7-[2-(morpholin-4-yl)ethyl]-6,7-dihydro-1H-purin-6-one
Smiles: O=C1NC(NCC2=CC(Cl)=C(Cl)C=C2)=NC2N=CN(CCN3CCOCC3)C=21
InChiKey: DEGSGBKTODESHH-UHFFFAOYSA-N
InChi: InChI=1S/C18H20Cl2N6O2/c19-13-2-1-12(9-14(13)20)10-21-18-23-16-15(17(27)24-18)26(11-22-16)4-3-25-5-7-28-8-6-25/h1-2,9,11H,3-8,10H2,(H2,21,23,24,27)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (147.65 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Ibezapolstat binds to and inhibits DNA pol IIIC from aerobic and low G+C Gram-positive bacteria. Ibezapolstat displays antibacterial activities against broad spectrum of C. difficile pathogens, with an MIC range of 1-8 μg/mL for a panel of 104 clinical isolates of C. difficile overall in vitro.
In Vivo:
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.
Products are for research use only. Not for human use.
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