MAC-545496
规格
| Cas Number | 838810-96-1 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 84 mg/mL (200.05 mM); Water: ˂1 mg/mL Ethanol: ˂1 mg/mL |
| 简短描述 | 抗感染抑制剂 |
| 英文简短描述 | Anti-infection Inhibitors |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | MAC-545496是一种纳摩尔级糖肽抗性相关蛋白R（GraR）抑制剂，与全长GraR蛋白具有很强的结合亲和力（Kdu2009≤\u20090.1\u2009nM）。MAC-545496 能逆转耐甲氧西林菌株对β-内酰胺类药物的耐药性，并能与 CAMPs 协同作用。MAC-545496在巨噬细胞中显示出显著的活性，并能减弱金黄色葡萄球菌幼虫感染模型中的毒力。 |
| 英文描述 |
Information MAC-545496 MAC-545496 is a nanomolar glycopeptide-resistance-associated protein R(GraR) inhibitor with strong binding affinity to the full-length GraR protein (Kd ≤ 0.1 nM). MAC-545496 can reverse β-lactam resistance in methicillin-resistant strains and synergize with CAMPs. MAC-545496 shows remarkable activity in macrophages and attenuates S. aureus virulence in a G. mellonella larvae infection model. Targets GraR (Cell-free assay) 0.1 nM(Kd) In vitro MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the half-maximal inhibitory concentration (IC50) is 0.0376\u2009µg/mL—matching with the concentration range of the synergistic effect with cefuroxime. MAC-545496 only inhibits the citrate-induced biofilm formation in the wild type in a concentration-dependent manner, suggesting additional potential as a lead for drug discovery. Treatment of S. aureus-infected macrophages with different doses of MAC-545496 added 30\u2009min after phagocytosis shows that the MAC-545496 halts S. aureus replication within macrophages starting at 0.5\u2009µg/mL.. In vivo MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponds to concentration-dependent killing of S. aureus in the hemolymph of the larvae observed from the CFUs recovered from the hemolymph 200\u2009min after infection. This matchs with the attenuated virulence of the graR::Tn mutant relative to the wild type in Galleria. Treatment with MAC-545496 recapitulates the phenotype of ΔgraR and ΔgraS mutants, effectively inhibiting intracellular S. aureus growth.. Cell Research(from reference) Cell lines：RAW macrophages Concentrations：20\u2009µg/mL Incubation Time：12 h |