2. Anti-infection Metabolic Enzyme/Protease
  3. Bacterial Aminoacyl-tRNA Synthetase
  4. Epetraborole hydrochloride

Epetraborole hydrochloride  (Synonyms: GSK2251052 hydrochloride)

Cat. No.: HY-12479A Purity: 99.63%
COA Handling Instructions

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Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research.

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

Epetraborole hydrochloride Chemical Structure

Epetraborole hydrochloride Chemical Structure

CAS No. : 1234563-16-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 154 In-stock
Solution
10 mM * 1 mL in DMSO USD 154 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 140 In-stock
10 mg USD 230 In-stock
25 mg USD 510 In-stock
50 mg USD 690 In-stock
100 mg USD 950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Epetraborole hydrochloride Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research[1][2][3].

IC50 & Target

IC50: 0.31 μM (LeuRS)[3]
In Vitro

Epetraborole (0-32 μg/mL) shows anti-bacterial activity against key gram-negative aerobic and anaerobic pathogens and gram-positive anaerobes[1].

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

Epetraborole hydrochloride Related Antibodies

Cell Viability Assay[1]

Cell Line: Anaerobes isolates
Concentration: 0-32 μg/mL
Incubation Time:
Result: Showed MIC50/MIC90 for all anaerobes isolates tested of 2 and 4 μg/mL, respectively.
Clinical Trial
Molecular Weight

273.52

Formula

C11H17BClNO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OCCCOC1=C(B(O)O[C@@H]2CN)C2=CC=C1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (731.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 28 mg/mL (102.37 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6560 mL 18.2802 mL 36.5604 mL
5 mM 0.7312 mL 3.6560 mL 7.3121 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.5 mg/mL (9.14 mM); Clear solution

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.14 mM); Clear solution

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (365.60 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.63%

COA (251 KB) LCMS (261 KB)

Handling Instructions (2659 KB)
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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 3.6560 mL 18.2802 mL 36.5604 mL 91.4010 mL
5 mM 0.7312 mL 3.6560 mL 7.3121 mL 18.2802 mL
10 mM 0.3656 mL 1.8280 mL 3.6560 mL 9.1401 mL
15 mM 0.2437 mL 1.2187 mL 2.4374 mL 6.0934 mL
20 mM 0.1828 mL 0.9140 mL 1.8280 mL 4.5700 mL
25 mM 0.1462 mL 0.7312 mL 1.4624 mL 3.6560 mL
30 mM 0.1219 mL 0.6093 mL 1.2187 mL 3.0467 mL
40 mM 0.0914 mL 0.4570 mL 0.9140 mL 2.2850 mL
50 mM 0.0731 mL 0.3656 mL 0.7312 mL 1.8280 mL
60 mM 0.0609 mL 0.3047 mL 0.6093 mL 1.5233 mL
80 mM 0.0457 mL 0.2285 mL 0.4570 mL 1.1425 mL
100 mM 0.0366 mL 0.1828 mL 0.3656 mL 0.9140 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Epetraborole hydrochloride 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:

Epetraborole1234563-16-6GSK2251052GSK 2251052GSK-2251052BacterialAminoacyl-tRNA SynthetasetRNA Synthetase, aaRSmultidrug-resistant gram-negative pathogens infectionanaerobes isolatesInhibitorinhibitorinhibit

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