MAC-545496 is potent GraR inhibitor (glycopeptide-resistance-associated protein R). MAC-545496 reverses β-lactam resistance in the community-acquired MRSA USA300 strain. MAC-545496 could also serve as an antivirulence agent alone; it attenuates MRSA virulence in Galleria mellonella larvae. MAC-545496 inhibits biofilm formation and abrogates intracellular survival in macrophages. Mechanistic characterization revealed MAC-545496 to be a nanomolar inhibitor of GraR, a regulator that responds to cell-envelope stress and is an important virulence factor and determinant of antibiotic resistance. MAC-545496 has value as a research tool to probe the GraXRS regulatory system and as an antibacterial lead series of a mechanism to combat drug-resistant Staphylococcal infections.
MedKoo Cat#: 555768
Name: MAC-545496
CAS#: 838810-96-1 (free base)
Chemical Formula: C18H18ClN5O3S
Exact Mass: 419.0819
Molecular Weight: 419.88
Elemental Analysis: C, 51.49; H, 4.32; Cl, 8.44; N, 16.68; O, 11.43; S, 7.64
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 167.0 | 397.73 |
The following data is based on the product molecular weight 419.88 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
