Epetraborole hydrochloride

• CAT Number: I000933
• CAS Number: 1234563-16-6
• Molecular Formula: C11H16BNO4 • HCl
• Molecular Weight: 273.50
• Purity: ≥95%
• Synonyms: 3-[[(3S)-3-(aminomethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl]oxy]-1-propanol, monohydrochloride
• Target: Synthases/Synthetases
• Solubility: H2O ≥ 28 mg/mL
• Storage: Store at -20°C
• IUPAC Name: 3-[[(3S)-3-(aminomethyl)-1-hydroxy-3H-2,1-benzoxaborol-7-yl]oxy]propan-1-ol;hydrochloride
• InChI: InChI=1S/C11H16BNO4.ClH/c13-7-10-8-3-1-4-9(16-6-2-5-14)11(8)12(15)17-10;/h1,3-4,10,14-15H,2,5-7,13H2;1H/t10-;/m1./s1
• InChIKey: DADYQGIQOBJGIW-HNCPQSOCSA-N
• SMILES: B1(C2=C(C=CC=C2OCCCO)[C@H](O1)CN)O.Cl

Epetraborole hydrochloride（Cat No.:I000933）is an investigational antibiotic belonging to the benzoxaborole class, specifically designed to combat mycobacterial infections, including non-tuberculous mycobacteria (NTM) and Mycobacterium avium complex (MAC) infections. It works by inhibiting leucyl-tRNA synthetase, an enzyme essential for protein synthesis in bacteria, ultimately leading to cell death. Epetraborole hydrochloride is particularly valuable for treating drug-resistant strains, offering a potential option for patients with limited therapeutic alternatives. Its unique mechanism and efficacy in preclinical and early clinical trials highlight its promise as a novel treatment for challenging mycobacterial infections.

Reference

[1]. Goldstein EJ et al. Comparative in vitro activities of GSK2251052, a novel boron-containing leucyl-tRNA synthetase inhibitor, against 916 anaerobic organisms.
Antimicrob Agents Chemother. 2013 May;57(5):2401-4.

[2]. O/’Dwyer K et al. Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment ofcomplicated urinary tract infections. Antimicrob Agents Chemother. 2015 Jan;59(1):289-98.