| Bioactivity | 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]. |
| Invitro | 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. 0 --> Antimicrobial agent-34 相关抗体: Cell Viability Assay[1] Cell Line: |
| 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: |
| Formula | C32H52N2O3 |
| Molar Mass | 512.77 |
| 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]. Fangquan Liu, et al. Design, synthesis and biological evaluation of amphiphilic benzopyran derivatives as potent antibacterial agents against multidrug-resistant bacteria. Eur J Med Chem. 2024 Nov 5:277:116784. |