DS86760016|cas:1853176-89-2|西域试剂

DS86760016

产品编号：Bellancom-124679| CAS NO：1853176-89-2| 分子式：C₉H₁₁BClNO₄| 分子量：243.45

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-124679		￥10000.00	杭州北京（现货）
Bellancom-124679		￥16000.00	杭州北京（现货）

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DS86760016

产品介绍

DS86760016 是一种亮氨酸-tRNA 合成酶 (LeuRS) 抑制剂，对多药耐药 (MDR) 革兰氏阴性菌, 如大肠杆菌、肺炎克雷伯菌和铜绿假单胞菌，具有抗菌活性。DS86760016 对大肠杆菌、铜绿假单胞菌和鲍曼不动杆菌的 LeuRS 酶有抑制作用，IC₅₀ 分别为 0.38、0.62 和 0.16 μM。

生物活性

DS86760016 is a potent leucyl-tRNA synthetase (LeuRS) inhibitor with activity against multidrug-resistant (MDR) Gram-negative bacteria, such as Escherichia coli, Klebsiella pneumoniae, and Pseudomonas aeruginosa. DS86760016 inhibits LeuRS enzymes from Escherichia coli, Pseudomonas aeruginosa, and Acinetobacter baumannii, with IC₅₀s of 0.38, 0.62, and 0.16 μM, respectively.

体外研究

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 MIC₉₀ of 2 μg/ml.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

DS86760016 (7.5-220 mg/kg; s.c.; q6h for 7 days) shows moderate spontaneous resistance (FSR).
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_IVs) of 1.5, 0.6, 3.7, and 3.0 μg h kg/ml/mg in mice, rats, monkeys, and dogs, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Immunocompetent female Swiss Webster mice (urinary tract infection, UTI model)
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Immunocompetent female Swiss Webster mice (urinary tract infection, UTI model)
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.