| Bioactivity | AU1235, an adamantyl urea, is a potent MmpL3 inhibitor. The Mycobacterium tuberculosis protein MmpL3 performs an essential role in cell wall synthesis, since it effects the transport of trehalose monomycolates across the inner membrane[1][2]. | ||||||||||||
| Invitro | AU1235 is similarly active against MDR isolates of M. tb displaying resistance to isoniazid, rifampicin, and pyrazinamide in addition to streptomycin, fluoroquinolones and/or ethambutol. AU1235 also inhibits Mycobacterium smegmatis and Mycobacterium fortuitum although the MICs (3.2 to 6.4 μg/ml) are significantly higher than against M. tb and M. bovis BCG[2]. | ||||||||||||
| Name | AU1235 | ||||||||||||
| CAS | 1338780-86-1 | ||||||||||||
| Formula | C17H19F3N2O | ||||||||||||
| Molar Mass | 324.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. McNeil MB, et al. Multiple Mutations in Mycobacterium tuberculosis MmpL3 Increase Resistance to MmpL3 Inhibitors. mSphere. 2020;5(5):e00985-20. Published 2020 Oct 14. [2]. Grzegorzewicz AE, et al. Inhibition of mycolic acid transport across the Mycobacterium tuberculosis plasma membrane. Nat Chem Biol. 2012;8(4):334-341. Published 2012 Feb 19. |