化合物 T10236L T10236L

Product Introduction
Bioactivity


英文名: ACHN-975

描述: ACHN-975 is a highly potent and selective LpxC inhibitor, demonstrating subnanomolar inhibitory activity. It effectively targets a broad spectrum of gram-negative bacteria, with low minimum inhibitory concentration (MIC) values (≤1 μg/mL)[1].

体外活性: ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM[1] and is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively[1]. ACHN-975 is against six P. aeruginosa isolates, it against P. aeruginosa APAE1064, APAE1232, and APAE1064 isolates with MIC values of 0.12, 0.06 and 0.06 ?μg/ml, respectively[2], it against Pseudomonas aeruginosa with an MIC50 and MIC90 of 0.06 and 0.25?μg/ml, respectively[2]. ACHN-975 is potently against the P. aeruginosa isolates tested, inhibiting 100% of the isolates at an MIC of ≤2?μg/ml. LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis and is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase[1].

体内活性: ACHN-975 (intraperitoneal administration; 5-30?mg/kg; single dose) leads to a steady reduction in bacterial titers in the first 4?h following treatment for all dosing groups, which shows that the level of free drug in this model drops below the ACHN-975 MIC for this isolate (0.25?μg/ml) by 2?h after treatment with the 10 mg/kg dose and by 4?h after treatment with the 30 mg/kg dose[2].

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

关键字: ACHN-975 | ACHN 975 | ACHN975

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途