Ibezapolstat
Based on 4 publication(s) in Google Scholar
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).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.0%
- CAS 番号: 1275582-97-2
- 分子式: C18H20Cl2N6O2
- 分子量:423.30
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Ibezapolstat
MoreDNA/RNA Synthesis アイソフォーム固有の製品をすべて表示
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生物活性
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DNA Polymerase |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ibezapolstat (50 mg/kg; p.o.; twice daily; for 3 days) shows strong anti-C. difficile properties in the hamster CDAD model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female golden Syrian hamsters (80-90 g), CDAD model[3]
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Dosage:50 mg/kg
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Administration:Oral administration, twice daily, for 3 days
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Result:Completely protected C. difficile-infected animals for a period of up to 5 days.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1275582-97-2
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性状 Solid
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分子量 423.30
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分子式 C18H20Cl2N6O2
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Color White to off-white
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SMILES
O=C1NC(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C1N(CCN4CCOCC4)C=N3
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別名
ACX-362E; GLS-362E
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (4)
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Journal Impact Factor
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Most Recent
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Expert Opin Investig Drugs
2025 Oct 28:1-17. PMID: 41117146 -
BMC Gastroenterol
In vitro susceptibility of clinical Clostridioides difficile isolates in Israel to metronidazole, vancomycin, fidaxomicin, ridinilazole and ibezapolstat. [Abstract]2025 Mar 31;25(1):209. PMID: 40165093 -
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溶剤 & 溶解度
DMSO : 62.5 mg/mL (147.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (275 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[3]. Sofya Dvoskin, et al. A Novel Agent Effective against Clostridium difficile Infection. Antimicrob Agents Chemother. 2012 Mar; 56(3): 1624-1626. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3624 mL | 11.8120 mL | 23.6239 mL | 59.0598 mL |
| 5 mM | 0.4725 mL | 2.3624 mL | 4.7248 mL | 11.8120 mL | |
| 10 mM | 0.2362 mL | 1.1812 mL | 2.3624 mL | 5.9060 mL | |
| 15 mM | 0.1575 mL | 0.7875 mL | 1.5749 mL | 3.9373 mL | |
| 20 mM | 0.1181 mL | 0.5906 mL | 1.1812 mL | 2.9530 mL | |
| 25 mM | 0.0945 mL | 0.4725 mL | 0.9450 mL | 2.3624 mL | |
| 30 mM | 0.0787 mL | 0.3937 mL | 0.7875 mL | 1.9687 mL | |
| 40 mM | 0.0591 mL | 0.2953 mL | 0.5906 mL | 1.4765 mL | |
| 50 mM | 0.0472 mL | 0.2362 mL | 0.4725 mL | 1.1812 mL | |
| 60 mM | 0.0394 mL | 0.1969 mL | 0.3937 mL | 0.9843 mL | |
| 80 mM | 0.0295 mL | 0.1476 mL | 0.2953 mL | 0.7382 mL | |
| 100 mM | 0.0236 mL | 0.1181 mL | 0.2362 mL | 0.5906 mL |
Ibezapolstat 関連分類
HY-128357 関連分類
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