Epetraborole
Based on 2 publication(s) in Google Scholar
Epetraborole (GSK2251052) is a leucyl-tRNA synthetase (LeuRS) inhibitor (IC50=0.31 μM), thereby inhibiting protein synthesis. Epetraborole can be used in multidrug-resistant gram-negative pathogens infection research.
For research use only. We do not sell to patients.
- CAS No.: 1093643-37-8
- Formula: C11H16BNO4
- Molecular Weight:237.06
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Epetraborole
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Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:Anaerobes isolates
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Concentration:0-32 μg/mL
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Incubation Time:
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Result:Showed MIC50/MIC90 for all anaerobes isolates tested of 2 and 4 μg/mL, respectively.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1093643-37-8
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Molecular Weight 237.06
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Formula C11H16BNO4
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SMILES
OCCCOC1=C2C([C@H](OB2O)CN)=CC=C1
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Synonyms
GSK-2251052; AN 3365
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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Antimicrob Agents Chemother
Activity of Oral Tebipenem-Avibactam in a Mouse Model of Mycobacterium abscessus Lung Infection. [Abstract]2023 Feb 16;67(2):e0145922. PMID: 36688684 -
Antimicrob Agents Chemother
2021 Sep 17;65(10):e0115621. PMID: 34280020
Protocols
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
Purity & Documentation
References
[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. [Content Brief]
[2]. O'Dwyer K, et al. 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. [Content Brief]
[3]. Sutcliffe JA. Antibiotics in development targeting protein synthesis. Ann N Y Acad Sci. 2011 Dec;1241:122-52. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)