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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
Epetraborole hydrochloride (also known as GSK2251052 hydrochloride and AN3365 hydrochloride) is a novel, potent and selective leucyl-tRNA synthetase (LeuRS) inhibitor, which inhibits protein synthesis by binding to the terminal adenosine ribose (A76) of leucyl-tRNA synthetase. Epetraborole was under investigation 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.
Targets |
LeuRS(IC50= 0.31 μM)
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ln Vitro |
Key gram-negative aerobic and anaerobic pathogens as well as gram-positive anaerobes are susceptible to the antibacterial action of epetraborole (0-32 μg/mL)[1].
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Cell Assay |
Cell Line: Anaerobes isolates
Concentration: 0-32 μg/mL Result: revealed MIC50/MIC90 values of 2 and 4 μg/mL for every anaerobe isolate tested. |
References |
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Molecular Formula |
C11H17BCLNO4
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Molecular Weight |
273.5210
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Elemental Analysis |
C, 48.30; H, 6.26; B, 3.95; Cl, 12.96; N, 5.12; O, 23.40
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CAS # |
1234563-16-6
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Related CAS # |
1234563-16-6 (HCl);1093643-37-8;1234563-15-5 (R-mandelate);
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Appearance |
Solid powder
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SMILES |
Cl[H].O1B(C2C(=C([H])C([H])=C([H])C=2[C@@]1([H])C([H])([H])N([H])[H])OC([H])([H])C([H])([H])C([H])([H])O[H])O[H]
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InChi Key |
DADYQGIQOBJGIW-HNCPQSOCSA-N
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InChi Code |
InChI=1S/C11H16BNO4.ClH/c13-7-10-8-3-1-4-9(16-6-2-5-14)11(8)12(15)17-10;/h1,3-4,10,14-15H,2,5-7,13H2;1H/t10-;/m1./s1
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Chemical Name |
(S)-3-(Aminomethyl)-7-(3-hydroxypropoxy)-1-hydroxy-1,3-dihydro-2,1-benzoxaborole hydrochloride
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Synonyms |
Epetraborole hydrochloride; GSK-2251052; GSK 2251052; GSK2251052; AN3365; AN 3365; AN-3365; GSK-052; GSK 052; GSK052;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~200 mg/mL (~731.21 mM)
H2O : ≥ 28 mg/mL (~102.37 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.14 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.14 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 5% DMSO+40% PEG300+5% Tween-80+50% Saline: ≥ 2.5 mg/mL (9.14 mM) Solubility in Formulation 4: 100 mg/mL (365.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.