MAC-545496

Research use only, not for human use.

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 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.

——

GPCR/G Protein

Antibacterial

——

——

——

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

——

(-20℃)

With Ice Pack

≥ 2 years