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DS86760016

产品编号 T39296 CAS 1853176-89-2

DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.

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DS86760016, CAS 1853176-89-2

规格	价格/CNY		货期	数量
25 mg	￥ 10,600		6-8周

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	DS86760016 is a highly effective inhibitor of leucyl-tRNA synthetase (LeuRS), demonstrating potent activity against multidrug-resistant (MDR) Gram-negative bacteria including Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. Notably, DS86760016 effectively inhibits LeuRS enzymes derived from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, exhibiting IC50 values of 0.38 μM, 0.62 μM, and 0.16 μM, respectively.
体外活性	DS86760016 inhibits some Gram-negative bacteria with an MICs ranging from 0.25 to 2 μg/ml. The MIC of DS86760016 against Gram-positive bacteria is >32 μg/ml. DS86760016 is active against both susceptible and these MDR P. aeruginosa , E. coli , and K. pneumoniae strains, with an MIC 90 of 2 μg/ml[1].
体内活性	DS86760016 (7.5-220 mg/kg; s.c.; q6h for 7 days) shows moderate spontaneous resistance (FSR)[1]. The pharmacokinetic (PK) parameters of DS86760016 in mouse, rat, monkey, and dog plasma by the intravenous (i.v.) route are test. DS86760016 shows lower intravenous plasma clearances (CL p ) of 11, 29, 5.6, and 4.5 ml/min/kg in mouse, rat, monkey, and dog plasma, respectively. The plasma half-lives (t 1/2 ) for DS86760016 are 1.9, 1.5, 8.6, and 8.3 h in mice, rats, monkeys, and dogs, respectively. The lower plasma clearance resulted in higher plasma exposures for DS86760016, with dose-normalized areas under the curve after i.v. administration (DNAUC IV s) of 1.5, 0.6, 3.7, and 3.0 μg h kg/ml/mg in mice, rats, monkeys, and dogs, respectively[1]. Animal Model: Immunocompetent female Swiss Webster mice (urinary tract infection, UTI model)[1]Dosage: 7.5, 30, 220 mg/kg Administration: S.c.; q6h for 7 days Result: Bacteria resistant to DS86760016 were detected in a few animals after 1 day of treatment at doses of 7.5 and 30 mg/kg q6h; however, no resistant bacteria were detected at these doses after 7 days of treatment. No resistance was observed in any of the mice treated at a dose of 220 mg/kg q6h.

分子量	243.45
分子式	C9H11BClNO4
CAS No.	1853176-89-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Purnapatre KP, et al. In Vitro and In Vivo Activities of DS86760016, a Novel Leucyl-tRNA Synthetase Inhibitor for Gram-Negative Pathogens. Antimicrob Agents Chemother. 2018;62(4):e01987-17. Published 2018 Mar 27. 2. Kumar M, et al. DS86760016, a Leucyl-tRNA Synthetase Inhibitor with Activity against Pseudomonas aeruginosa. Antimicrob Agents Chemother. 2019;63(4):e02122-18. Published 2019 Mar 27.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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