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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-LPC-233
LPC-233

Chemical Structure : LPC-233

CAS No.: 2142075-09-8

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LPC-233 (LPC233)

货号: PC-21019Not For Human Use, Lab Use Only.

LPC-233 (LPC233) is a highly potent and specific inhibitor of UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC (Ki=8.9 pM), specifically inhibits lipid A synthesis and displays outstanding antibiotic activities.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LPC-233 (LPC233) is a highly potent and specific inhibitor of UDP-3-O-(R-3-hydroxyacyl)-N-acetylglucosamine deacetylase LpxC (Ki=8.9 pM), specifically inhibits lipid A synthesis and displays outstanding antibiotic activities.
LPC-233 is a competitive inhibitor occupying the active site and substrate binding passage against the P. aeruginosa LpxC.
LPC-233 exhihits KI value of 0.22 ± 0.06 nM and 8.9 ± 0.5 pM for the encounter complex EI and stable complex EI*, respectively.
LPC-233 is broadly effective against a clinical collection of 285 strains of Gram-negative bacterial pathogens (MIC90<1.0 ug/mL), does not display detectable antibiotic activity toward Gram-positive bacteria, such as S. aureus, at 128 μg/mL.
LPC-233 has an MIC50 value of 0.064 μg/ml and an MIC90 value of 0.125 μg/ml against 151 extended spectrum β-lactamase (ESBL)–negative, carbapenemase-negative Enterobacteriaceae isolates.
LPC-233 displays identical MIC50 and MIC90 values against 42 ESBL, carbapenemase-producing isolates that are resistant to antibiotics.
LPC-233 does not substantially inhibit human MMPs (MMP-1, MMP-2, MMP-3, MMP-7, MMP-8. MMP-9, MMP-12, MMP-13, and MMP-14) and TACE at 30 uM.
LPC-233 demonstrates in vivo efficacy in multiple murine infection models, displays no cardiovascular toxicity in vivo.

物理化学性质&存储条件

分子量 376.36
分子式 C19H18F2N2O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

O=C(N[C@H](C(NO)=O)[C@](C)(O)C(F)F)C1=CC=C(C#CC#CC2CC2)C=C1

参考文献

1. Jinshi Zhao, et al. Sci Transl Med. 2023 Aug 9;15(708):eadf5668.

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