2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Anti-infection Cell Cycle/DNA Damage
  3. Reactive Oxygen Species (ROS) Bacterial ClpP
  4. Anti-MRSA agent 39

Anti-MRSA agent 39 是一种口服有效的 ClpX 调节剂，能以高亲和力 (Kd = 3.6 μM) 与金黄色葡萄球菌酪蛋白水解酶 X (SaClpX) 结合。Anti-MRSA agent 39 通过温度依赖性抑制细胞分裂发挥抗菌作用。Anti-MRSA agent 39 可引起 MRSA 的显著代谢紊乱，表现为 ATP 水平显著降低、活性氧 (ROS) 水平升高、NAD+/NADH 比值下降，并加速耐甲氧西林金黄色葡萄球菌 (MRSA) ATCC 33591 的裂解速率。Anti-MRSA agent 39 能显著增加处于有丝分裂期的 MRSA 细胞的比例，并使细胞出现明显的形态异常。Anti-MRSA agent 39 可用于侵袭性 MRSA 感染的研究。

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Anti-MRSA agent 39

Anti-MRSA agent 39 Chemical Structure

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Anti-MRSA agent 39 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anti-MRSA agent 39 is an orally active ClpX modulator that binds Staphylococcus aureus caseinolytic protease X (SaClpX) with high affinity (Kd = 3.6 μM). Anti-MRSA agent 39 exerts antibacterial effects through temperature-dependent inhibition of cell division. Anti-MRSA agent 39 elicits profound metabolic dysregulation in methicillin-resistant Staphylococcus aureus (MRSA), manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591. Anti-MRSA agent 39 significantly increases the proportion of MRSA cells in the mitotic phase, and the cells exhibit obvious morphological abnormalities. Anti-MRSA agent 39 can be used for the study of invasive MRSA infections[1].

体外研究
(In Vitro)

Anti-MRSA agent 39 (Compound 13) (18-72 小时) 对 MRSA 表现出强效抑制活性 (MIC = 1 μg/mL)，且对人肝细胞系 LO2 无明显毒性 (IC50 = 8.15 μM)[1]。
Anti-MRSA agent 39 (0.25-1 μg/mL，0-12 小时) 能以浓度依赖的方式快速清除 MRSA，并在 4 倍 MIC 浓度下于 12 小时内将细菌载量降低至无法检测的水平[1]。
与万古霉素相比，Anti-MRSA agent 39 诱导耐药突变的倾向显著降低[1]。
Anti-MRSA agent 39 (100 μM，30 分钟) 能稳定 SaClpX 六聚体结构并减少二聚体/三聚体的形成[1]。
Anti-MRSA agent 39 显著上调 MRSA ATCC 33591 中 ftsZ mRNA 的表达水平[1]。
Anti-MRSA agent 39 在30 ℃ 时 MIC 值降低 2-4 倍，这种“负温度系数”特征与 MRSA ATCC 33591 中ClpX 分子伴侣的活性相符[1]。
Anti-MRSA agent 39 (0.25-0.5 μg/mL，1-5 小时) 引起 MRSA 代谢的显著紊乱，表现为 ATP 水平显著降低、活性氧 (ROS) 水平升高、NAD+/NADH比值下降，并加速 MRSA ATCC 33591 的裂解速率[1]。

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

Anti-MRSA agent 39 相关抗体:
体内研究
(In Vivo)

Anti-MRSA agent 39 (Compound 13) (5-1000 mg/kg，口服一次；皮下注射，每日一次，持续 3 天) 在小鼠 MRSA 皮肤感染模型中显著降低了细菌载量和病变大小，有效抑制了 MRSA 感染，促进了伤口愈合，并且在剂量 ≤ 750 mg/kg 时显示出良好的安全性[1]。

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

Animal Model: Male BALB/c mice (8-week-old)[1].
Dosage: 500 mg/kg, 750 mg/kg, 1000 mg/kg
Administration: P.o., once
Result: A decrease in body weight on the second day and a 50 % mortality rate were observed within the first five days.
At the doses of 750 mg/kg and 500 mg/kg, no toxic reactions or mortalities were observed throughout the experiment.
The 750 mg/kg dosage group demonstrated a transient decrease in body weight on the second day; subsequently, their body weights gradually recovered from the fifth day post-administration.
Showed mild liver and kidney inflammation in the 1000 mg/kg and 750 mg/kg dose groups.
No significant organ damage in the major organs of the mice.
Animal Model: A skin abscess model was established in male BALB/c mice (8-week-old) by subcutaneous injection of 60 μL of MRSA bacterial suspension (1 × 107 CFU/mL)[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: S.c., once daily for 3 days
Result: Exhibited a substantial recovery in body weight, enhanced wound healing, and a significant reduction in lesion size and subsidence rate.
Exhibited a reduction in bacterial content within the skin of the mice.
Exhibited no discernible pathological alterations, maintaining a well-defined skin structure and minimal inflammatory cell infiltration.
分子量

338.20

Formula

C18H12BrNO
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

Anti-MRSA agent 39 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Anti-MRSA agent 39Reactive Oxygen Species (ROS)BacterialClpPCaseinolytic protease PMethicillin-Resistant Staphylococcus aureusMRSAClpXInhibitorinhibitorinhibit

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