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编 号:F762601
分子式:C28H35F3N4O3
分子量:532.6
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生物活性:
(R)-ZG197 is a highly selective Staphylococcus aureus Caseinolytic protease P (SaClpP) activator with an EC50 of 1.5?μM. (R)-ZG197 also activates Homo sapiens ClpP (HsClpP) with an EC50 of 31.4 μM.

体内研究:
(R)-ZG197 (25-100 mg/kg; i.p.; once) 显著延长斑马鱼 USA300 感染模型的存活率。(R)-ZG197 (7.5 mg/kg; s.c.; twice a day for 3 days) 在小鼠皮肤 S. aureus 感染模型中显示抗感染功效。Animal Model:Zebrafish USA300 infection model
Dosage:25, 50, or 100?mg/kg
Administration:Intraperitoneal injection, single dose
Result:Significantly prolong the survival rate at 50 mg/kg. Lost therapeutic effects on zebrafish infected with the ΔclpP mutant strain.
Animal Model:Female BALB/c mice, S. aureus infection model
Dosage:7.5?mg/kg
Administration:Subcutaneous injection, twice a day for 3 days
Result:Caused a smaller necrotic lesion size in mice compared with the vehicle control.

体外研究:
(R)-ZG197 (10?μM; 2 h) 显著提高 SaClpP 的热稳定性,而对 HsClpP 影响较弱。(R)-ZG197 (0-256 μg/mL; 18 h) 显著抑制 S. aureus,MIC 为 0.5 μg/mL。(R)-ZG197 对 S. aureus 表现出较强的、广谱的抗菌活性,MIC 值为 0.5-2 μg/mL。(R)-ZG197 (0-20 μM) 在 8325-4 S. aureus 中降低 SaFtsZ 丰度,在 ΔclpP 突变株中则没有相应效果。
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