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Art. -Nr.: HY-12479

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Epetraborole

(Synonyms: GSK-2251052; AN 3365)

2 Cited Publications

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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.

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CAS. Nr.: 1093643-37-8

Formel: C₁₁H₁₆BNO₄

Molecular Weight:237.06

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

Epetraborole Chemical Structure

CAS. Nr.: 1093643-37-8

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Data Download

Data Sheet (273 KB)

Handling Instructions (2659 KB)

Other Forms of Epetraborole:

Epetraborole hydrochloride
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Epetraborole (R-mandelate)
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Top Publications Citing

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Publications Citing Use of MedChemExpress (MCE) Epetraborole
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Antimicrob Agents Chemother. 2023 Feb 16;67(2):e0145922. [Abstract]

Antimicrob Agents Chemother. 2021 Sep 17;65(10):e0115621. [Abstract]

Biologische Aktivität

Beschreibung

IC₅₀ & Target

In Vitro

Clinical Trial

Chemical Information

Publications (2)

Reinheit & Dokumentation

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Bioz

Biologische Aktivität

Beschreibung

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^[1]^[2]^[3].

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.

Cell Viability Assay^[1]

Cell Line:

Anaerobes isolates

Concentration:

0-32 μg/mL

Incubation Time:

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

A549

NCT01329991 Plexxikon| 2011-05 PHASE1

Chemical Information

CAS. Nr. 1093643-37-8

Molecular Weight 237.06

Formel C₁₁H₁₆BNO₄

SMILES

OCCCOC1=C2C([C@H](OB2O)CN)=CC=C1

Synonyms

GSK-2251052; AN 3365

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (2)

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Most Recent

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

Epetraborole Is Active against Mycobacterium abscessus. [Abstract]

2021 Sep 17;65(10):e0115621. PMID: 34280020

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)

COA (2659 KB)

Elemental Analysis Report (2659 KB)

HNMR (2659 KB)

CNMR (2659 KB)

RP-HPLC (2659 KB)

NP-HPLC (2659 KB)

MS (2659 KB)

LCMS (2659 KB)

IR (2659 KB)

GC (2659 KB)

OR (2659 KB)

SDS-PAGE (2659 KB)

SEC-HPLC (2659 KB)

Other Report (2659 KB)

Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

=
Konzentration Konzentration

×
Volumen Volumen

×
Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

×

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

=

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

×

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Epetraborole Related Classifications

HY-12479 Related Classifications

Anti-infection Metabolic Enzyme/Protease

Bacterial Aminoacyl-tRNA Synthetase

Infection

Powered by Bioz See more details on Bioz

Keywords

Epetraborole
1093643-37-8
GSK-2251052
AN 3365
GSK2251052
GSK 2251052
AN3365
AN 3365
AN-3365
Bacterial
Aminoacyl-tRNA Synthetase
multidrug-resistant gram-negative pathogens infection
anaerobes isolates
Inhibitor
inhibitor
inhibit

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Epetraborole

2 Cited Publications

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NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

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