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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
838810-96-1
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥830.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥380.0 |
| 规格： | 5 mg | 产品价格： | ￥750.0 |
| 规格： | 10 mg | 产品价格： | ￥1200.0 |
| 规格： | 25 mg | 产品价格： | ￥2200.0 |
| 规格： | 50 mg | 产品价格： | ￥3500.0 |
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MAC-545496
CAS No. : 838810-96-1
MCE 国际站：MAC-545496
产品活性：MAC-545496 是糖肽抗性相关蛋白 R (GraR) 的纳摩尔抑制剂。MAC-545496 对全长 GraR 蛋白具有很强的结合亲和力 (Kd ≤ 0.1 nM)。 MAC-545496 是一种抗毒剂，可逆转耐甲氧西林的菌株 (MRSA) 中的 β-内酰胺耐药性。
研究领域：Anti-infection
作用靶点：Bacterial
In Vitro: MAC-545496 potently synergizes with Cefuroxime; concentrations as low as 0.03 µg/mL (~75 nM) lowers the β-lactam MIC from 512 to 8 µg/mL against S. aureus USA300. MAC545496 also synergizes with Cefuroxime and Oxacillin against a collection of ten S. aureus clinical isolates. In addition, MAC-545496 potentiates the effect of Cefuroxime against representatives of other circulating MRSA strains such as USA100, USA400 and USA500 to different extents, with the exception of CMRSA4, a USA200/EMRSA16 isolate. MAC-545496 also synergizes with the antimicrobial peptides colistin and polymyxin B.
MAC-545496 shows inhibition of mprF expression in a concentration-dependent manner; the IC50 value is 0.0376 µg/mL.
MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner.
In Vivo: In vivo, MAC-545496 is effective as a monotherapy for MRSA infected Galleria mellonella larvae. MAC-545496 activity is evidenced by increased survival of the drug-treated larvae as compared to infected untreated ones. This corresponded 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. Treatment of S. aureus-infected larvae with MAC-545496 occurred 30min after infection that mimics acquiring bacterial infection before initiating antimicrobial therapy .
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