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ACX-362E is an orally bioavailable DNA polymerase IIIC (pol IIIC) inhibitor, acts as an antimicrobial agent to treat Gram-positive infections, with a MIC50 of 2 μg/mL for C. difficile. ACX-362E exhibits very potent in vitro and in vivo activities against broad spectrum of C. difficile pathogens.
| ln Vitro |
Ibezapolstat binds to and inhibits DNA pol IIIC of aerobic and low-G+C Gram-positive bacteria[1]. Ibezapolstat exhibits broad-spectrum antibacterial action against C. difficile pathogens, with in vitro MICs ranging from 1-8 μg/mL against 104 C. difficile clinical isolates [1].
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| ln Vivo |
In a hamster model of Clostridium difficile-associated disease (CDAD), ibezapolstat is poorly absorbed and appears harmless (with the potential to achieve high local concentrations at sites of C. difficile infection in the colon) [3]. Ibezabolostat (oral; 50 mg/kg; twice daily; for 3 days) exhibits strong anti-C properties. difficult characteristics in a CDAD model of hamsters [3].
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| Animal Protocol |
Animal/Disease Models: Female Syrian golden hamster (80-90 g), CDAD model [3]
Doses: 50 mg/kg Route of Administration: Orally, twice (two times) daily for 3 days Experimental Results: Complete protection of C. difficile-infected animals, sustained A period of up to 5 days. |
| References |
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| Additional Infomation |
Ibezapolstat is under investigation in clinical trial NCT04247542 (ACX-362E [Ibezapolstat] for Oral Treatment of Clostridioides Difficile Infection).
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| Molecular Formula |
C18H20CL2N6O2
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|---|---|
| Molecular Weight |
423.2964
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| Exact Mass |
422.102
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| CAS # |
1275582-97-2
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| PubChem CID |
136022209
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| Appearance |
White to off-white solid powder
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| LogP |
1.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
588
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C(C=CC(=C1)CNC1=NC2=C(C(N1)=O)N(C=N2)CCN1CCOCC1)Cl
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| InChi Key |
DEGSGBKTODESHH-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-[(3,4-dichlorophenyl)methylamino]-7-(2-morpholin-4-ylethyl)-1H-purin-6-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~147.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3624 mL | 11.8120 mL | 23.6239 mL | |
| 5 mM | 0.4725 mL | 2.3624 mL | 4.7248 mL | |
| 10 mM | 0.2362 mL | 1.1812 mL | 2.3624 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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