ACHN-975 TFA|1410809-37-8|-陌孚医药/Medlife

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ACHN-975 TFA

目录号: PL12217 纯度: ≥95.0%

CAS No. :1410809-37-8

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中文名称	ACHN-975 TFA
英文名称	ACHN-975 TFA
英文别名	ACHN-975 TFA;(2S)-3-amino-N-hydroxy-2-[(4-{4-[(1R,2R)-2-(hydroxymethyl)cyclopropyl]buta-1,3-diyn-1-yl}phenyl)formamido]-3-methylbutanamide, trifluoroacetic acid;N-[(2S)-3-amino-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yl]-4-[4-[(1R,2R)-2-(hydroxymethyl)cyclopropyl]buta-1,3-diynyl]benzamide;2,2,2-trifluoroacetic acid;Z2768390156;(2S)-3-amino-N-hydroxy-2-[(4-{4-[(1R,2R)-2-(hydroxymethyl)cyclopropyl]buta-1,3-diyn-1-yl}phenyl)f
Cas No.	1410809-37-8
分子式	C₂₂H₂₄F₃N₃O₆
分子量	483.44
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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。

生物活性

ACHN-975 TFA is a selective LpxC inhibitor and exhibits a subnanomolar LpxC inhibitory activity. ACHN-975 TFA is against a wide range of gram-negative bacterias with low MIC values (≤1 μg/mL).

性状

Solid

IC50 & Target[1][2]

IC50: LpxC

体外研究(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-dependen

体内研究(In Vivo)

ACHN-975 TFA (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.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Kalinin DV, et al. Insights into the Zinc-Dependent Deacetylase LpxC: Biochemical Properties and Inhibitor Design. Curr Top Med Chem. 2016;16(21):2379-430.
[2]. Krause KM,et al. Potent LpxC Inhibitors with In Vitro Activity against Multidrug-Resistant Pseudomonas aeruginosa.Antimicrob Agents Chemother. 2019 Oct 22;63(11). pii: e00977-19.

溶解度数据	In Vitro: DMSO : 100 mg/mL (206.85 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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