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AN3365 (hydrochloride) (Synonyms: Epetraborole,GSK2251052)

Catalog No.GC12345

에페트라보롤(GSK2251052) 염산염은 새로운 류실-tRNA 합성효소(LeuRS) 억제제(IC50=0.31 μM)로 단백질 합성을 억제합니다.

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AN3365 (hydrochloride) Chemical Structure

Cas No.: 1234563-16-6

Size 가격 재고 수량
10mM (in 1mL DMSO)
US$129.00
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1mg
US$54.00
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5mg
US$117.00
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10mg
US$189.00
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25mg
US$329.00
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50mg
US$495.00
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Sample solution is provided at 25 µL, 10mM.

Description of AN3365 (hydrochloride)

AN3365 is a potent and selective leucyl-tRNA synthetase inhibitor [1].

The leucyl-tRNA synthetase belongs to a member of the class I aminoacyl-tRNA synthetase family. The leucyl-tRNA synthetase has been involved in catalyzing the ATP-dependent ligation of L-leucine to tRNA. It has been found in the cytoplasm as part of a multisynthetase complex and interacts with the arginine tRNA synthetase through its C-terminal domain [2].

AN3365 potently and selectively inhibited bacterial leucyl-tRNA synthetase activity against Gram-negative bacteria. AN3365 was a member of a novel class of boron-containing compounds, the aminomethyl benzoxoaboroles, which showed potential to combat multidrug resistance. AN3365 was active against many microbial strains, including strains of Enterobacteriaceae with the MIC50/90 of 0.5/1 μg/ml. AN3365 showed activity against the non-fermentative Gram-negative clinical isolates P. aeruginosa, A. baumannii, S. maltophilia, and B. cepacid with the MIC50/90s of 4/8, 4/8, 2/4, and 8/32 μg/ml, respectively [1].

References:
[1] Hernandez V, Crépin T, Palencia A, et al.  Discovery of a novel class of boron-based antibacterials with activity against gram-negative bacteria[J]. Antimicrobial agents and chemotherapy, 2013, 57(3): 1394-1403.
[2] Rouget P, Chapeville F.  Leucyl‐tRNA Synthetase[J]. European journal of biochemistry, 1971, 23(3): 443-451.

Chemical Properties of AN3365 (hydrochloride)

Cas No. 1234563-16-6 SDF
Synonyms Epetraborole,GSK2251052
Chemical Name 3-[[(3S)-3-(aminomethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaborol-7-yl]oxy]-1-propanol, monohydrochloride
Canonical SMILES OB1O[C@H](CN)C2=CC=CC(OCCCO)=C21.Cl
Formula C11H16BNO4 • HCl M.Wt 273.5
Solubility ≤10mg/ml in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AN3365 (hydrochloride)

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1 mg 5 mg 10 mg
1 mM 3.6563 mL 18.2815 mL 36.5631 mL
5 mM 0.7313 mL 3.6563 mL 7.3126 mL
10 mM 0.3656 mL 1.8282 mL 3.6563 mL
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In vivo Formulation Calculator (Clear solution) of AN3365 (hydrochloride)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Review for AN3365 (hydrochloride)

Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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