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[CAS NO. 1234563-16-6] Epetraborolehydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-12479A |
| Brand: | MCE |
| CAS: | 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 |
2 Publications Citing Use of MCE
Summary
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
DMSO : 200 mg/mL ( 731.21 mM ; Need ultrasonic)
H 2 O : ≥ 28 mg/mL ( 102.37 mM )
* "≥" means soluble, but saturation unknown.
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 |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (365.60 mM); Clear solution; Need ultrasonic
-
2.
-
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
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.
- [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.
- [3] Sutcliffe JA. Antibiotics in development targeting protein synthesis. Ann N Y Acad Sci. 2011 Dec;1241:122-52.
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