2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial DNA/RNA Synthesis
  4. Ibezapolstat

Ibezapolstat  (Synonyms: ACX-362E; GLS-362E)

Cat. No.: HY-128357 Purity: ≥98.0%
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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).

For research use only. We do not sell to patients.

Ibezapolstat Chemical Structure

Ibezapolstat Chemical Structure

CAS No. : 1275582-97-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 154 In-stock
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5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 460 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Ibezapolstat:

Ibezapolstat Related Antibodies

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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)[1][2].

IC50 & Target

Ki: 0.325 μM (DNA pol IIIC from C. difficile)[2]
In Vitro

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 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female golden Syrian hamsters (80-90 g), CDAD model[3]
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.
Clinical Trial
Molecular Weight

423.30

Formula

C18H20Cl2N6O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC(NCC2=CC=C(Cl)C(Cl)=C2)=NC3=C1N(CCN4CCOCC4)C=N3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Ibezapolstat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ibezapolstat1275582-97-2ACX-362E GLS-362EBacterialDNA/RNA SynthesisClostridiumdifficileinfectionCDIreplication-specificDNApolymeraseInhibitorinhibitorinhibit

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