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DS86760016

CAS No. : 1853176-89-2

MCE 站：DS86760016

产品活性：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。

研究领域：Anti-infection

作用靶点：Bacterial

In Vitro: 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.

In Vivo: 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.

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