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首页-小分子抑制剂&激动剂-Antibiotics and Antivirals-Bacterial-(R)-ZG197
(R)-ZG197

Chemical Structure : (R)-ZG197

CAS No.: 2999672-72-7

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(R)-ZG197

货号: PC-23552Not For Human Use, Lab Use Only.

(R)-ZG197 is a highly selective S. aureus caseinolytic protease P (SaClpP) activator / agonist with EC50 of 1.5 uM and Kd of 58 nM in BLI assays, 20-fold higher activity than that activates HsClpP.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

(R)-ZG197 is a highly selective S. aureus caseinolytic protease P (SaClpP) activator / agonist with EC50 of 1.5 uM and Kd of 58 nM in BLI assays, 20-fold higher activity than that activates HsClpP.
(R)-ZG197 selectively binds to and activates SaClpP but not HsClpP.
(R)-ZG197 activates SaClpP to degrade α-casein and SaFtsZ in vitro. promote the degradation of cellular SaFtsZ protein in cell lysates of S. aureus 8325-4 clpP knockout (ΔclpP) strain with the supplement of the recombinant SaClpP protein, but no SaFtsZ degradation occurred in the presence of the recombinant HsClpP protein.
(R)-ZG197 exhibits antibacterial activity in a SaClpP-dependent manner, significantly suppresses S. aureus with a quantified MIC of 0.5 μg/mL.
(R)-ZG197 displays strong antibacterial activity on a broad spectrum of S. aureus USA300, NRS-1, NRS-70, NRS-100, NRS-108, and NRS-271 MRSA strains.
(R)-ZG197 demonstrates promising antibiotic efficacy in zebrafish and murine skin infection models.

物理化学性质&存储条件

分子量 532.61
分子式 C28H35F3N4O3
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

(6S,9aS)-6-((S)-sec-butyl)-8-((R)-1-(naphthalen-1-yl)ethyl)-4,7-dioxo-N-(4,4,4-trifluorobutyl)hexahydro-2H-pyrazino[1,2-a]pyrimidine-1(6H)-carboxamide

参考文献

1. Wei B, et al. Nat Commun. 2022 Nov 14;13(1):6909.

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