MAC-545496

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

MAC-545496 is a nanomolar inhibitor of glycopeptide-resistance-associated protein R (GraR). MAC-545496 displays strong binding affinity to the full-length GraR protein (Kd ● 0.1 nM).

MAC-545496 potently synergizes with Cefuroxime; concentrations as low as 0.03 ┢g/mL (~75 nM) lowers the ┑-lactam MIC from 512 to 8 ┢g/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 ┢g/mL.MAC-545496 also inhibits the citrateinduced biofilm formation in the wild type in a concentration dependent manner.

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GPCR/G Protein

Antibacterial

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838810-96-1

419.89

C18H18ClN5O3S

>98% (HPLC)

DMSO : 250 mg/mL (595.39 mM; Need ultrasonic)

O=C(NC(NC1=NC=C(Cl)C=C1)=S)C2=CC=C(N3CCCCC3)C([N+]([O-])=O)=C2

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(-20℃)

With Ice Pack

≥ 2 years