Bioactivity | (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[1]. |
Target | EC50: 1.5 μM (SaClpP), 31.4 μM (HsClpP)Kd: 2.5 μM (SaClpP) |
Invitro | (R)-ZG197 (10 μM; 2 h) 显著提高 SaClpP 的热稳定性,而对 HsClpP 影响较弱[1]。(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[1]。(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[1]。 Western Blot Analysis[1] Cell Line: |
In Vivo | (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[1]。(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[1]。 Animal Model: |
Name | (R)-ZG197 |
Formula | C28H35F3N4O3 |
Molar Mass | 532.60 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Wei B, et al. Anti-infective therapy using species-specific activators of Staphylococcus aureus ClpP. Nat Commun. 2022 Nov 14;13(1):6909. |