[CAS NO. 1234563-16-6] Epetraborolehydrochloride

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PRODUCTS SPECIFICATIONS [1234563-16-6]

Catalog

HY-12479A

Brand

MCE

CAS

1234563-16-6

DESCRIPTION [1234563-16-6]

Overview

MDL	MFCD30343855
Molecular Weight	273.52
Molecular Formula	C11H17BClNO4
SMILES	OCCCOC1=C(B(O)O[C@@H]2CN)C2=CC=C1.[H]Cl

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

Epetraborole (GSK2251052) hydrochloride is a novel leucyl-tRNA synthetase ( LeuRS ) inhibitor ( IC ₅₀ =0.31 μM), thereby inhibiting protein synthesis. Epetraborole hydrochloride can be used in multidrug-resistant gram-negative pathogens infection research ^[1] ^[2] ^[3] .

IC50 & Target

IC ₅₀ : 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] .

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 MIC ₅₀ /MIC ₉₀ for all anaerobes isolates tested of 2 and 4 μg/mL, respectively.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01381562	GlaxoSmithKline	Infections, Intestinal	October 3, 2011	Phase 2
NCT05283746	AN2 Therapeutics, Inc	Renal Insufficiency	February 21, 2022	Phase 1
NCT01495065	GlaxoSmithKline	Community-acquired Infection	December 19, 2011	Phase 1
NCT01381549	GlaxoSmithKline	Infections, Urinary Tract	June 28, 2011	Phase 2
NCT05327803	AN2 Therapeutics, Inc	MAC Lung Disease\|Treatment Refractory MAC Lung Disease	May 20, 2022	Phase 2\|Phase 3
NCT04892641	AN2 Therapeutics, Inc	Healthy Volunteers	June 10, 2021	Phase 1
NCT01262885	GlaxoSmithKline	Infections, Bacterial	October 7, 2010	Phase 1
NCT01702350	GlaxoSmithKline	Community-acquired Infection	October 21, 2011	Phase 1
NCT01475695	GlaxoSmithKline	Community-acquired Infection	April 21, 2011	Phase 1
NCT01267968	GlaxoSmithKline	Community-acquired Infection	January 11, 2011	Phase 1

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL ( 731.21 mM ; Need ultrasonic)

H ₂ O : ≥ 28 mg/mL ( 102.37 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.6560 mL	18.2802 mL	36.5604 mL
5 mM	0.7312 mL	3.6560 mL	7.3121 mL
10 mM	0.3656 mL	1.8280 mL	3.6560 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 100 mg/mL (365.60 mM); Clear solution; Need ultrasonic
2.

Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

Solubility: ≥ 2.5 mg/mL (9.14 mM); Clear solution
3.

Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (9.14 mM); Clear solution

* All of the co-solvents are available by MCE.