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Epetraborole hydrochloride

Chemical Structure : Epetraborole hydrochloride

CAS No.: 1234563-16-6

Epetraborole hydrochloride (GSK2251052 hydrochloride, AN3365)

Catalog No.: PC-43054Not For Human Use, Lab Use Only.

Epetraborole hydrochloride (GSK2251052, AN3365) is a broad-spectrum antibacterial inhibitor of leucyl tRNA-synthetase (LeuRS), shows MIC50/MIC90 of 2/4 ug/ml against 916 clinical anaerobic isolates.

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Biological Activity

Epetraborole hydrochloride (GSK2251052, AN3365) is a broad-spectrum antibacterial inhibitor of leucyl tRNA-synthetase (LeuRS), shows MIC50/MIC90 of 2/4 ug/ml against 916 clinical anaerobic isolates.
Epetraborole has MIC90s against 302 Bacteroides fragilis and Bacteroides thetaiotaomicron strains are 4 and 8 μg/ml, respectively.
A single amino acid polymorphism (P329) within the editing domain of LeuRS reduces susceptibility to GSK2251052.

Physicochemical Properties

M.Wt 273.521
Formula C11H17BClNO4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

H2O: ≥ 28 mg/mL

Chemical Name/SMILES

1-Propanol, 3-[[(3S)-3-(aminomethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl]oxy]-, hydrochloride (1:1)

References

1. Goldstein EJ, et al. Antimicrob Agents Chemother. 2013 May;57(5):2401-4.

2. Tenero D, et al. Antimicrob Agents Chemother. 2013 Jul;57(7):3334-9.

3. O'Dwyer K, et al. Antimicrob Agents Chemother. 2015 Jan;59(1):289-98.

4. Gupta A, et al. Antimicrob Agents Chemother. 2016 Apr 22;60(5):3219-21.

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