PA-824
PA-824, a bicyclic nitroimidazoles, is an anti-tuberculosis (TB) agent that exerts potent in vitro activity against Mycobacterium tuberculosis with the minimal inhibition concentration (MIC) ranging from 0.015 μg/ml to 0.25 μg/ml and remains actively against a wide range of isolates that are resistant to commonly used anti-TB agents leading to its successful application in the treatment of TB [1].
PA-824 has been found to exhibit bactericidal activity against replicating bacilli and non-replicating bacilli under hypoxic or prolonged culture conditions in a dose dependent fashion through two possible mechanisms, which include PA-824 induced inhibition of ketomycolate synthesis and PA-824 mediated donation of nitric oxide during enzymatic nitro-reduction [1].
References:
[1] Ahmad Z, Peloquin CA, Singh RP, Derendorf H, Tyagi S, Ginsberg A, Grosset JH, Nuermberger EL. PA-824 exhibits time-dependent activity in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011 Jan;55(1):239-45. doi: 10.1128/AAC.00849-10. Epub 2010 Oct 11.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 359.26 |
| Cas No. | 187235-37-6 |
| Formula | C14H12F3N3O5 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥17.85 mg/mL in DMSO |
| Chemical Name | (6S)-2-nitro-6-[[4-(trifluoromethoxy)phenyl]methoxy]-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine |
| SDF | Download SDF |
| Canonical SMILES | C1C(COC2=NC(=CN21)[N+](=O)[O-])OCC3=CC=C(C=C3)OC(F)(F)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | PA-824 is an anti-tuberculosis drug with MIC value of < 2.8 μM. | |||||
| Targets | tuberculosis | |||||
| IC50 | <2.8 μM | |||||
Quality Control & MSDS
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Chemical structure
