Ridinilazole-SMT19969-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERidinilazoleCat. No.: HY-16753CAS No.: 308362-25-6Synonyms: SMT19969分式: CHN分量: 388.42作靶點(diǎn): Bacterial作通路: Anti-infection儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 60 mg/mL (154.47 mM)* m

2、eans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.5745 mL 12.8727 mL 25.7453 mL5 mM 0.5149 mL 2.5745 mL 5.1491 mL10 mM 0.2575 mL 1.2873 mL 2.5745 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Ridinilazole種新型的抗 劑，作于 C. difficile，MIC 范圍為 0

3、.06-0.25 g/mL (MIC90=8g/mL)。IC50 & Target MIC90: 8g/mL (C.difficile) 1體外研究Ridinilazole is a novel antibacterial that does not appear to act through the classical pathways associated1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEwith antibiotics, such as inhibition of cell wall, protein, lipid, RNA

4、 or DNA synthesis. Ridinilazole may impaircell division. Ridinilazole is bactericidal against C.difficile and exhibits a prolonged post-antibiotic effect. Insusceptibility testing of 82 clinical isolates of C.difficile (including ribotype 027), Ridinilazole displays potentgrowth inhibition and has l

5、ower MICs MIC range, 0.06-0.25g/mL; MIC for 90% of the organisms (MIC90),0.125g/mL than Metronidazole (MIC range, 0.125-8g/mL; MIC90, 8g/mL) or Vancomycin (MIC range,0.5-4g/mL; MIC90, 2g/mL). Similarly, Ridinilazole is found to be more potent than Metronidazole orVancomycin at inhibiting the growth

6、of 50 ribotype-defined C.difficile strains. The activity of Ridinilazoleagainst specific C.difficile ribotypes (including ribotypes 001, 002, 005, 014, 027, 054 and 106) is similar,with an MIC range of 0.060.5g/mL and an MIC90 of 0.125g/mL. In addition, Ridinilazole is more activeagainst 11 ribotype

7、 027 strains than either Metronidazole or Vancomycin 1.體內(nèi)研究 In a hamster model of CDI with a once-daily dosing regimen, Ridinilazole displays greater efficacy thanVancomycin both against non-epidemic and epidemic strains of C.difficile. Similar to the twice-daily dosingstudy, plasma levels of Ridini

8、lazole are below the level of detection, whereas caecal Ridinilazoleconcentrations are well above the MIC, thus demonstrating the non-absorbable nature of Ridinilazole andminimal systemic exposure 1.REFERENCES1. Vickers RJ, et al. Ridinilazole: a novel therapy for Clostridium difficile infection. Int J Antimicrob Agents. 2016 Aug;48(2):137-43.McePdfHeightCaution: Product has not been fully validated for medical applicatio