2. Anti-infection Cell Cycle/DNA Damage
  3. Bacterial ClpP
  4. ClpP agonist 1

ClpP agonist 1 是一种金黄色葡萄球菌 ClpP (SaClpP) 激动剂，其 EC50 为 1.44 μM，Kd 值为 2.95 μM (等温滴定量热法) 和 18 μM (生物膜层干涉技术)，具有低耐药频率。ClpP agonist 1 在小鼠皮肤感染模型中能降低细菌载量、缩小感染面积并改善组织病理学结果。ClpP agonist 1 可用于耐 Methicillin (HY-121544) 金黄色葡萄球菌 (MRSA) 皮肤感染的研究。

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ClpP agonist 1

ClpP agonist 1 Chemical Structure

CAS No. : 2761081-10-9

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ClpP agonist 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ClpP agonist 1 is a Staphylococcus aureus ClpP (SaClpP) agonist with an EC50 of 1.44 μM, Kd values of 2.95 μM (isothermal titration calorimetry) and 18 μM (bio-layer interferometry), and a low drug resistance frequency. ClpP agonist 1 reduces bacterial load, shrinks infected area and improves histopathological outcomes in a mouse skin infection model. ClpP agonist 1 can be used for the research of Methicillin (HY-121544)-resistant Staphylococcus aureus (MRSA) skin infections[1].

体外研究
(In Vitro)

ClpP agonist 1 (Compound Z1) (0.06-128 μg/mL; 18 h) 对 MRSA ATCC 33591 表现出强效抗菌活性，其 MIC 为 0.5 μg/mL，且该活性依赖于 SaClpP 的存在[1]。
ClpP agonist 1 (72 h) 对 HepG2 细胞表现出细胞毒性，其 IC50 为 3.10 μM[1]。

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

ClpP agonist 1 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route AUC0-t MRT0-t T1/2 Tmax CL Cmax Bioavailability
Mice[1] 5 mg/kg i.v. 1955.2 ng·h/mL 1.09 h 0.81 h / 2.55 L/h/kg 1982.5 ng/mL /
Mice[1] 10 mg/kg p.o. 1310.5 ng·h/mL 2.29 h 1.92 h 0.75 h 7.30 L/h/kg 432 ng/mL 33.5 %
体内研究
(In Vivo)

ClpP agonist 1 (Compound Z1) (2.5-10 mg/kg；皮下注射；每日一次；连续 3 天) 对 BALB/c 小鼠的 MRSA 皮肤感染表现出显著的、剂量依赖性治疗效果，可缩小病损面积、降低细菌载量并减轻组织病理损伤，且在测试剂量下具有良好的安全性特征[1]。

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

Animal Model: BALB/c (female, 6-8 weeks old, 18-20 g, SPF grade)[1]
Dosage: 2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration: s.c.; daily; 3 consecutive days
Result: Showed no statistically significant differences in body weight compared to the vehicle group, with no compound-related adverse effects noted.
Reduced lesion size from baseline significantly in a dose-dependent manner.
Decreased MRSA load in skin tissues remarkably compared to the vehicle group, with the 10 mg/kg dose group showing the most pronounced reduction.
Markedly alleviated tissue damage, including reduced epidermal necrosis, dermal thickening, and inflammatory cell infiltration, while preserving normal histological architecture.
分子量

476.44

Formula

C24H21F5N4O
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

ClpP agonist 1 相关分类

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  • 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.

Keywords:

ClpP agonist 12761081-10-9ClpP agonist1ClpP agonist-1BacterialClpPCaseinolytic protease PMRSA ATCC 33591S. aureus 8325methicillin-resistant staphylococcus aureusmurine skin infection modelBALB/c miceStaphylococcus aureusHepG2 cellsα-caseinmiceStaphylococcus aureus ClpPInhibitorinhibitorinhibit

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