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CHIR-090 目录号:GY04167 特价

CAS号:728865-23-4

分子式:C24H27N3O5

分子量:437.49

CHIR-090是一种大肠杆菌 LpxC 抑制剂,Ki 为 4nM。

规格 价格/RMB 库存 购买数量
2mg 1148 有库存
5mg 1779 有库存
10mg 2818 有库存
50mg 7591 有库存
大包装询价!

产品仅用于科研,严禁用于临床

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生物活性实验指南文献化学信息溶解性

生物活性(数据来源于公开文献,仅供参考)

产品简述 CHIR-090是一种大肠杆菌 LpxC 抑制剂,Ki 为 4nM。
靶点 & IC50
Escherichia coli LpxC
4 nM (Ki)[1]
细胞 & 酶实验结果 CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase from the hyperthermophile Aquifex aeolicus, and it has excellent antibiotic activity against P. aeruginosa and E. coli, as judged by disk diffusion assays. CHIR-090 is also a two-step slow, tight-binding inhibitor of Escherichia coli LpxC with Ki=4 nM. CHIR-090 at low nM levels inhibits LpxC orthologues from diverse Gram-negative pathogens, including Pseudomonas aeruginosa, Neisseria meningitidis, and Helicobacter pylori. In contrast, CHIR-090 is a relatively weak competitive and conventional inhibitor (lacking slow, tight-binding kinetics) of LpxC from Rhizobium leguminosarum (Ki=340 nM), a Gram-negative plant endosymbiont that is resistant to this compound. An E. coli construct in which the chromosomal lpxC gene is replaced by R. leguminosarum lpxC is resistant to CHIR-090 up to 100 μg/mL, or 400 times above the minimal inhibitory concentration for wild-type E. coli. CHIR-090, a very potent, slow, tight-binding inhibitor of Aquifex aeolicus LpxC, the sequence of which is 31 % identical to E. coli LpxC. CHIR-090 has remarkable antibiotic activity against E. coli and P. aeruginosa, comparable to ciprofloxacin, as judged by disk diffusion assays[1].
动物实验结果 CHIR-090 is a potent antibiotic against E. coli and inhibits E. coli LpxC activity in vitro in the low nM range. E. coli W3110 colonies resistant to 1 μg/mL CHIR-090 are not observed without prior chemical mutagenesis. A strain of E. coli W3110 is able to grow on LB agar plates containing 1 to 10 μg/mL CHIR-090, which is 4 to 40 times above the MIC of 0.25 μg/mL under our conditions for wild-type E. coli W3110. The doubling time of W3110RL is 40 min in the presence of 1 μg/mL CHIR-090, which is exactly the same rate as wild-type in the absence of inhibitor. Wild-type cells stopped growing after about 2 h in the presence of 1 μg/mL CHIR-090[1].

实验指南

激酶实验[1]
Kinase Assay
Disk diffusion is conducted, except that 10 μg of each antibiotic compound is used per filter. Growth in liquid medium in the presence of CHIR-090 is evaluated as follows: cells from overnight cultures are inoculated into 50 mL portions of LB broth at an A600 of 0.02 and grown with shaking at 30°C. When the A600 reaches 0.15, parallel cultures are treated with either 6 μL of 500 μg/mL CHIR-090 in DMSO or 6 μL of DMSO. To assess cumulative growth, cultures are maintained in log phase growth by 10-fold dilution into pre-warmed medium, containing the same concentrations of DMSO or DMSO/CHIR-090, whenever the A600 reaches 0.4. The minimal inhibitory concentration is defined as the lowest antibiotic concentration at which no measurable bacterial growth is observed in LB medium containing 1% DMSO (v/v), when inoculated at a starting density of A600=0.01. Cultures are incubated with shaking for 24 h at 30°C in the presence of CHIR-090. Experiments are performed in triplicate[1]. 
细胞实验:
细胞株
浓度
孵化时间
实验方法
动物实验:
动物模型
剂型
剂量
给药方式

化学信息

CAS号 728865-23-4
分子式 C24H27N3O5
分子量 437.49
稳定性 粉末,-20°C,2年;DMSO溶剂,4°C,2周;DMSO溶剂,-80°C,6个月

溶解性(仅供参考)

体内实验溶剂
动物实验剂型
由于生产工艺和批次不同,溶解性可能会有所差异。

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