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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 (K_d ≤ 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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