Bioactivity | 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)[1][2]. | ||||||||||||
Target | Ki: 0.325 μM (DNA pol IIIC from C. difficile) | ||||||||||||
Invitro | Ibezapolstat binds to and inhibits DNA pol IIIC from aerobic and low G+C Gram-positive bacteria[1].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[1]. | ||||||||||||
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)[3].Ibezapolstat (50 mg/kg; p.o.; twice daily; for 3 days) shows strong anti-C. difficile properties in the hamster CDAD model[3]. Animal Model: | ||||||||||||
Name | Ibezapolstat | ||||||||||||
CAS | 1275582-97-2 | ||||||||||||
Formula | C18H20Cl2N6O2 | ||||||||||||
Molar Mass | 423.30 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Beverly Murray, et al. In vitro activity of the novel antibacterial agent ibezapolstat (ACX-362E) against Clostridioides difficile. J Antimicrob Chemother. 2020 Aug 1;75(8):2149-2155. [2]. Andrea Torti, et al. Clostridium difficile DNA polymerase IIIC: basis for activity of antibacterial compounds. Curr Enzym Inhib. 2011 Oct; 7(3): 147-153. [3]. Sofya Dvoskin, et al. A Novel Agent Effective against Clostridium difficile Infection. Antimicrob Agents Chemother. 2012 Mar; 56(3): 1624-1626. |