Epetraborole, also known as GSK2251052 and AN3365, is a potent and selective leucyl-tRNA synthetase inhibitor. Epetraborole was in development for the treatment of infections caused by multidrug-resistant Gram-negative pathogens. GSK2251052 is a novel boron-containing antibiotic that inhibits bacterial leucyl tRNA synthetase. All Clostridium perfringens strains had GSK2251052 MICs of >32 μg/ml.
CAS Number: 1234563-16-6
Molecular Weight: 273.52
Chemical Name: (S)-3-(Aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole hydrochloride
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO, not in water
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
- O'Dwyer K, Spivak AT, Ingraham K, Min S, Holmes DJ, Jakielaszek C, Rittenhouse S, Kwan AL, Livi GP, Sathe G, Thomas E, Van Horn S, Miller LA, Twynholm M, Tomayko J, Dalessandro M, Caltabiano M, Scangarella-Oman NE, Brown JR. Bacterial resistance to leucyl-tRNA synthetase inhibitor GSK2251052 develops during treatment of complicated urinary tract infections. Antimicrob Agents Chemother. 2015 Jan;59(1):289-98. doi: 10.1128/AAC.03774-14. Epub 2014 Oct 27. PubMed PMID: 25348524; PubMed Central PMCID: PMC4291364.
- Wu L, Vogt FG, Liu DQ. Flow-injection MS/MS for gas-phase chiral recognition and enantiomeric quantitation of a novel boron-containing antibiotic (GSK2251052A) by the mass spectrometric kinetic method. Anal Chem. 2013 May 21;85(10):4869-74. doi: 10.1021/ac401079x. Epub 2013 May 7. PubMed PMID: 23650921.
- Tenero D, Bowers G, Rodvold KA, Patel A, Kurtinecz M, Dumont E, Tomayko J, Patel P. Intrapulmonary pharmacokinetics of GSK2251052 in healthy volunteers. Antimicrob Agents Chemother. 2013 Jul;57(7):3334-9. doi: 10.1128/AAC.02483-12. Epub 2013 May 6. PubMed PMID: 23650164; PubMed Central PMCID: PMC3697385.
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