生物活性 | |||
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描述 | GraR (glycopeptide-resistance-associated protein R), also known as ApsR (antimicrobial-peptide sensor protein R) is a response regulator protein of a multicomponent regulatory system including the sensor kinase GraS, a signal transduction accessory protein GraX that is associated with the ABC transporter VraFG. GraR is a regulator that responds to cell-envelope stress and is an important virulence factor and determinant of antibiotic resistance. MAC-545496 is a nanomolar inhibitor of GraR. MAC-545496 reverses β-lactam resistance in the community-acquired methicillin-resistant strains (MRSA) USA300 strain. MAC-545496 could also serve as an antivirulence agent alone; it attenuates MRSA virulence in Galleria mellonella larvae. MAC-545496 (~0.5 μg/mL) inhibits biofilm formation and abrogates intracellular survival in macrophages[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.38mL 0.48mL 0.24mL |
11.91mL 2.38mL 1.19mL |
23.82mL 4.76mL 2.38mL |
参考文献 |
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