您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > MRL-494
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MRL-494
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MRL-494图片
规格:98%
分子量:659.12
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MRL-494 是一种抗菌剂,是 BamA 的一种抗外排和外膜渗透屏障的小分子抑制剂。MRL-494 可抑制革兰氏阳性细菌 (金黄色葡萄球菌 COL 的 MIC 值为 12.5 μM) 和革兰氏阴性细菌 (大肠杆菌 JCM158 的 MIC 值为 25 μM)。
货号:ajcx29520
CAS:N/A
分子式:C26H35FN16O2
分子量:659.12
溶解度:N/A
纯度:98%
存储:Store at -20°C
库存:现货

Background:

MRL-494 is an antibacterial agent and is a small-molecule inhibitor of β-barrel assembly machine A (BamA) impervious to efflux and the outer membrane permeability barrier. MRL-494 can inhibits Gram-positive (MIC of 12.5 μM for Staphylococcus aureus COL) and Gram-negative (MIC of 25 μM for E. coli JCM158) bacterias[1][2].

The mutant protein has both altered conformation and activity, suggesting it could either inhibit MRL-494 binding or allow BamA to function in the presence of MRL-494. By cellular thermal shift assay (CETSA), MRL-494 stabilizes BamA and BamAE470K from thermally induced aggregation, indicating direct or proximal binding to both BamA and BamAE470K. It is the altered activity of BamAE470K responsible for resistance to MRL-494. MRL-494 possesses a second mechanism of action that kills gram-positive organisms. In microbes lacking an OM, MRL-494 lethally disrupts the cytoplasmic membrane. The compound cannot disrupt the cytoplasmic membrane of gram-negative bacteria because it cannot penetrate the OM. Instead, MRL-494 inhibits OMP biogenesis from outside the OM by targeting BamA[1].MRL-494 exhibits strong anti-microbial properties against both Gram-positive and Gram-negative bacteria. The MIC values of MRL-494 against E. coli (WT), E. coli (δtolC), E. coli (δtolC envA101), K. pneumonia, A. baumannii (WT), A. baumannii (δlpxC) , P. aeruginosa (efflux deficient), P. aeruginosa (WT), Staphylococcus aureus (methicillin-resistant) and Bacillus subtilis rpoB18 are 25 μM, 25 μM, 25 μM, 100 μM, 200 μM, 200 μM, 100 μM, 100 μM, 12.5 μM and 25 μM, respectively[2].


[1]. Hart EM, A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier. Proc Natl Acad Sci U S A. 2019 Oct 22;116(43):21748-21757. [2]. Hart EM, A small-molecule inhibitor of BamA impervious to efflux and the outer membrane permeability barrier. Proc Natl Acad Sci U S A. 2019 Oct 22;116(43):21748-21757.