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1410809-36-7
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ACHN-975
CAS No. : 1410809-36-7
MCE 国际站：ACHN-975
产品活性：ACHN-975 是细菌酶 LpxC 的选择性抑制剂，表现出亚纳摩尔级 LpxC 抑制活性。ACHN-975 对多种革兰氏阴性菌的 MIC 值低于 1 μg/mL。
研究领域：Anti-infection
作用靶点：Bacterial
In Vitro: ACHN-975 is against Enterobacteriaceae spp with an IC50 of 0.02 nM.
ACHN-975 is against Enterobacteriaceae spp, Pa, and Ab with MIC90 values of 1, 0.5, and >64 μg/mL, respectively.
ACHN-975 is potently against the P. aeruginosa isolates tested, inhibiting 100% of the isolates at an MIC of ≤2 μg/ml. It against Pseudomonas aeruginosa with an MIC50 and MIC90 of 0.06 and 0.25 μg/ml, respectively.
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.
LpxC is highly conserved in gram-negative bacteria and catalyzes the first committed step of lipid A biosynthesis. LpxC is the bacterial enzyme Zinc-dependent metalloamidase UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase.
In Vivo: 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. The sampling 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.
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文献和实验血氨及数字连接试验(NCT)。结果：治疗组治疗后血氨36 μmol.L-1±12 μmol.L-1,NCT 52 s±23 s；对照组血氨52 μmol.L-1±18 μmol.L-1，NCT 81 s±26 s(P＜0.01)。结论：乳果糖治疗SHE有效、方便、安全。 ［中图分类号］ R975.3;R575.2 ［文献标识码］ B ［文章编号］ 1007-7669(2000)06-0523-02 亚临床肝性脑病(subclinical hepatic
36.36ml 72.72ml 109.07ml 1000ml/ 98.15g/M 1M 2M 3M 4M 5M 6M 7M 8M KC2 H3 O2 [g] 98.15 196.3 294.45 392.6 490.75 588.9 687.05
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