[CAS NO. 2131798-13-3]  Ganfeborole hydrochloride

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PRODUCTS SPECIFICATIONS [2131798-13-3]

Distributor
Catalog
AS894390
Brand
Arctom Scientific
CAS
2131798-13-3

DESCRIPTION [2131798-13-3]

Overview

MDL-
Molecular Weight293.94
Molecular FormulaC10H14BCl2NO4
SMILESOB1O[C@H](CN)C2=C(Cl)C=CC(OCCO)=C21.[H]Cl

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


Summary

Ganfeborole hydrochloride (GSK656) is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis ( Mtb ) leucyl-tRNA synthetase (LeuRS) , with an IC 50 of 0.2 μM.


IC50 & Target

IC50: 0.2 μM ( Mtb LeuRS) [1]


In Vitro

Ganfeborole hydrochloride is highly selective inhibitor for Mycobacterium tuberculosis ( Mtb ) leucyl-tRNA synthetase (LeuRS), with an IC 50 of 0.2 μM, and shows IC 50 s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. Ganfeborole hydrochloride exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. Ganfeborole hydrochloride also exhibits EC 50 s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis [1] .

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


In Vivo

Ganfeborole hydrochloride shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED 99 of 0.4 mg/kg [1] .

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


Appearance

Solid


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 : 67.5 mg/mL ( 229.64 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4021 mL 17.0103 mL 34.0205 mL
5 mM 0.6804 mL 3.4021 mL 6.8041 mL
10 mM 0.3402 mL 1.7010 mL 3.4021 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

* All of the co-solvents are available by MCE.