1. Cell Cycle/DNA Damage Anti-infection
  2. ClpP Bacterial
  3. (R)-ZG197

(R)-ZG197 是一种高选择性的金黄色葡萄球菌酪蛋白溶解蛋白酶 P (SaClpP) 激活剂,其 EC50 为 1.5 μM。(R)-ZG197 也激活 Homo sapiens ClpP (HsClpP),EC50 为 31.4 μM。

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(R)-ZG197 Chemical Structure

(R)-ZG197 Chemical Structure

CAS No. : 2999672-72-7

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

EC50: 1.5 μM (SaClpP), 31.4 μM (HsClpP)[1]
Kd: 2.5 μM (SaClpP)[1]

体外研究
(In Vitro)

(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Cell lysates of S. aureus 8325-4 clpP knockout (ΔclpP) strain
Concentration: 0, 2.5, 5 and 10 μM
Incubation Time: 15 min
Result: SaFtsZ protein was degraded when SaClpP was added.
体内研究
(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]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zebrafish USA300 infection model[1]
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[1]
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.
分子量

532.60

Formula

C28H35F3N4O3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(R)-ZG197
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HY-152096
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