• 产品描述： MAC-545496是一种纳摩尔浓度的glycopeptide-resistance-associated protein R(GraR)抑制剂，对全长GraR蛋白(Kd≤0.1 nM)具有很强的结合亲和力。 MAC-545496可以逆转耐甲氧西林菌株中的β-内酰胺耐药性，并与CAMP协同作用。 MAC-545496在巨噬细胞中显示出显着的活性，并减弱了苜蓿根瘤菌幼虫感染模型中的金黄色葡萄球菌毒力

• 靶点： GraR(Cell-free assay):0.1 nM(Kd);Antibacterial

• 体内研究：
  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 min 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

• 细胞实验： Cell lines: RAW macrophages Concentrations: 20 µg/mL Incubation Time: 12 h Method: Stationary-phase cells are washed and diluted in serum-free RPMI (SF-RPMI) and used for infection of RAW macrophages at a multiplicity of infection of ten. One set of replicates for S. aureus USA300 contains MAC-545496 (20 µg/mL) so that the drug is present throughout every step of the experiment. Macrophages exposed to bacteria are centrifuged at 277g to synchronize infection and after 30 min at 37 °C in 5% CO2, the medium is replaced with SF-RPMI containing gentamicin (100 µg/mL) for 1 h. Here, after phagocytosis, another set of S. aureus USA300 replicates are exposed to MAC-545496 along with gentamicin so that the drug is added after the bacteria are phagocytosed. For wells already treated with MAC-545496, the drug is added too. After gentamicin treatment, one set of wells are lysed by treatment with 0.5 ml of 0.1% Triton X-100 after washing with PBS. The remaining well for each infection is incubated with RPMI containin

• 动物实验： Animal Models: Galleria mellonella larvae Dosages: 10 µL/100 mg Administration: IV

• 参考文献：
  1. El-Halfawy OM, et al. Nat Chem Biol. 2020;16(2):143-149.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.382 ml	11.908 ml	23.816 ml
  5 mM	0.476 ml	2.382 ml	4.763 ml
  10 mM	0.238 ml	1.191 ml	2.382 ml
  50 mM	0.048 ml	0.238 ml	0.476 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *