2. Anti-infection
  3. Bacterial
  4. Antimicrobial agent-34

Antimicrobial agent-34 (compound 4h) 是一种抗菌剂 (MIC = 1–4 μg/mL)，clogP 值为 9.14。Antimicrobial agent-34 血浆稳定性好 (HC50 为 131.1 μg/mL)，具有良好的膜选择性 (HC50/MIC 为 65.6)，具备快速杀菌能力。Antimicrobial agent-34 通过破坏细菌细胞膜完整性，诱导细胞内活性氧增加及蛋白质和 DNA 泄漏，最终导致细菌死亡。Antimicrobial agent-34 在金黄色葡萄球菌 ATCC43300 感染的小鼠败血症模型中，展现了显著的体内抗菌效力。

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Antimicrobial agent-34 Chemical Structure

Antimicrobial agent-34 Chemical Structure

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Antimicrobial agent-34 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

Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300[1].

体外研究
(In Vitro)

Antimicrobial agent-34 可在人血清，血浆和血液中稳定存在，MBC 分别为 16，16，32 μg/mL，没有失去抗菌作用[1]。
Antimicrobial agent-34 对 6 种革兰氏阳性菌的抑菌活性最强，抗菌谱宽，MIC 范围为 1-4 μg/mL，对肺炎克雷伯氏杆菌 ATCC10031，鲍曼氏杆菌 ATCC19606，大肠杆菌 ATCC25922 也有较好的抑菌活性，MIC 分别为4，2，4 μg/ mL[1]。
Antimicrobial agent-34 (1 ×-16 × MIC) 对金黄色葡萄球菌均表现出快速的抑菌活性，且有剂量依赖性[1]。
Antimicrobial agent-34 (2-16 mg/mL; 0-24 h) 难以诱导抗性，对金黄色葡萄球菌 ATCC43300 进行亚 MIC (1/2 MIC) 下的耐药测试，MIC 变化仅为 2-4 倍[1]。
Antimicrobial agent-34 (2-64 mg/mL，0-20 天) 有较强的抑制生物膜形成和破坏预形成生物膜的能力，且呈剂量依赖性[1]。
Antimicrobial agent-34 (2-32 mg/mL，0-20 min) 破坏金黄色葡萄球菌的跨膜电位，从而增加通透性，有效提高金黄色葡萄球菌中 ROS，DNA 和蛋白质水平[1]。

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

Antimicrobial agent-34 相关抗体:

Cell Viability Assay[1]

Cell Line: Staphylococcus aureus ATCC43300
Concentration: 2, 4, 8, 16 mg/mL
Incubation Time: 0, 2, 4, 6, 8, 10, 12, 20, 24 h
Result: Achieved a 8.35 log reduction (killing ≥99.9 % of S. aureus) in 4 h compared with the control, and the killing rate was 100 % after 8 h, while reference drug vancomycin exhibited a 8.55 log reduction of S. aureus within 8 h at the same concentration.

Cell Viability Assay[1]

Cell Line: Staphylococcus aureus ATCC43300
Concentration: 2, 4, 8, 16, 32, 64 mg/mL
Incubation Time: 20 days
Result: Inhibited the formation of biofilm of Staphylococcus aureus, and the formation of biofilm was significantly reduced with the increase of concentration. 8 μg/mL eliminated 26.69% of the established biofilm of Staphylococcus aureus, and the eradication rate of biofilm at 64 μg/mL exceeded 40%.
体内研究
(In Vivo)

Antimicrobial agent-34 (5 and 10 mg/kg，i.p.，continuously at 12-h intervals for 2 days) 对革兰氏阳性菌具有较强的体内抑制作用，使金黄色葡萄球菌 ATCC43300 感染的小鼠脓毒症模型中小鼠血液、肝、肾、脾等脏器细菌负荷明显降低，治疗后小鼠血液中 TNF-α，IL-6 降低[1]。

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

Animal Model: Mouse sepsis model infected by S. aureus ATCC43300[1].
Dosage: 5 and 10 mg/kg; continuously at 12-h intervals for 2 days
Administration: Intraperitoneal injection (i.p.)
Result: Achieved 1.10, 1.98, 2.00 and 2.09 log (91.8 %, 98.9 %, 99.0 % and 99.2 %) reductions in the number of surviving bacterial colonies in blood, liver, spleen and kidney by 5mg/mL.
Achieved, respectively, 1.46, 2.69, 2.24 and 2.84 log (95.9 %, 99.8 %, 99.4 % and 99.9 %) by 10mg/mL.
Decreased in the level of proinflammatory cytokines including TNF-α and IL-6.
分子量

512.77

Formula

C32H52N2O3
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

Antimicrobial agent-34 相关分类

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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.

Keywords:

Antimicrobial agent-34Antimicrobial agent34Antimicrobial agent 34BacterialBacterial resistanceMembrane-targetingAMPsInhibitorinhibitorinhibit

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