MUT056399 是一种金黄色葡萄球菌和大肠杆菌的 FabI 酶的高效抑制剂，IC50值分别为 12 nM 和 58 nM。

MUT056399 is a highly potent inhibitor of the FabI enzyme of both S. aureus and E. coli (IC50s of 12 nM and 58 nM, respectively).

MUT056399 is a highly potent new inhibitor of the FabI enzyme of both Staphylococcus aureus and Escherichia coli.?In vitro, MUT056399 was very active against S. aureus strains, including methicillin-susceptible S. aureus (MSSA), methicillin-resistant S. aureus (MRSA), linezolid-resistant, and multidrug-resistant strains, with MIC(90)s between 0.03 and 0.12 μg/ml.?MUT056399 was also active against coagulase-negative staphylococci, with MIC(90)s between 0.12 and 4 μg/ml.?The antibacterial spectrum is consistent with specific FabI inhibition with no activity against bacteria using FabK but activity against FabI-containing Gram-negative bacilli.?In vitro, resistant clones of S. aureus were obtained at a low frequency.?All of the resistant clones analyzed were found to contain mutations in the fabI gene[1].

In vivo, MUT056399, administered subcutaneously, protected mice from a lethal systemic infection induced by MSSA, MRSA, and vancomycin-intermediate S. aureus strains (50% effective doses ranging from 19.3 mg/kg/day to 49.6 mg/kg/day).?In the nonneutropenic murine thigh infection model, the same treatment with MUT056399 reduced the bacterial multiplication of MSSA and MRSA in the thighs of immunocompetent mice[1]

1269055-85-7

C15H13F2NO3

293.27

Fab-001

DMSO:30 mg/mL (102.29mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years