| Name | MUT056399 |
| Description | MUT056399 (Fab-001) is a highly potent inhibitor of the FabI enzyme in both S. aureus and E. coli, with IC50 values of 12 nM and 58 nM, respectively. |
| In vitro | 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 | 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 30 mg/mL (102.29 mM), Sonication is recommended.
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| Keywords | S. aureus | MUT-056399 | MUT056399 | MUT 056399 | Inhibitor | inhibit | Fab001 | Fab 001 | Bacterial |
| Inhibitors Related | Neomycin sulfate | Adipic dihydrazide | Levulinic acid | D(+)-Raffinose pentahydrate | Sulfamethoxazole sodium | Terbinafine hydrochloride | Doxycycline | Hyaluronic acid sodium (MW 20 kDa) | Dimethyl sulfoxide | Sodium diacetate | Sodium bicarbonate | BES |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Inhibitor Library | Anti-Bacterial Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Infection Compound Library |
United States
