Pretomanid-PA-824-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPretomanidCat. No.: HY-10844CAS No.: 187235-37-6Synonyms: PA-824; (S)-PA 824分式: CHFNO分量: 359.26作靶点: Bacterial作通路: Anti-infection储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 33 mg/mL (91.

2、86 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.7835 mL 13.9175 mL 27.8350 mL5 mM 0.5567 mL 2.7835 mL 5.5670 mL10 mM 0.2783 mL 1.3917 mL 2.7835 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Pretomanid (PA-824) 可作于肺结核，MIC为1 g/m

3、L。IC50 & Target Tuberculosis.体外研究Pretomanid (PA-824) exhibited a sub-micromolar minimal inhibitory concentration (MIC) against MTB,1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEAlthough Pretomanid (PA-824) was not the most potent NAP against cultured MTB clinical isolates, it was themost active i

4、n infected mice when orally administered at 25 mg/kg. This indicated that Pretomanid (PA-824)might possess more desirable pharmacokinetic properties than the other more potent NAP compounds thatwe tested. Further studies in mice at 25, 50 and 100 mg kg-1 Pretomanid (PA-824) daily for 10 days resulte

5、din reductions of mycobacterial burden in both spleen and lung tissues that were comparable to that of INH at25 mg kg -1 1. Pretomanid (PA-824) showed significant activity at 2, 10, and 50 microg/ml, similar to that ofmetronidazole, in a dose-dependent manner. Pretomanid (PA-824) at 100 mg/kg in cyc

6、lodextrin/lecithin wasas active as moxifloxacin at 100 mg/kg and isoniazid at 25 mg/kg and was slightly more active than rifampinat 20 mg/kg. Long-term treatment with Pretomanid (PA-824) at 100 mg/kg in cyclodextrin/lecithin reduced thebacterial load below 500 CFU in the lungs and spleen 2. Pretoman

7、id (PA-824) has no effect on the viabilityof M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase,encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule 3.REFERENCES1. Stover CK, et al. A small-molecule nit

8、roimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000 Jun22;405(6789):962-6.2. Lenaerts AJ, et al. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of invitro and in vivo models. Antimicrob Agents Chemother. 2005 Jun;49(6):2294-301.3. Manjunatha UH, et al. Mycobacterium leprae is naturally resistant to PA-824. Antimicrob Agents Chemother. 2006 Oct;50(10):3350-4.McePdfHeightCaution: Product has not been fully validated for medical appl