1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAzithromycinCat. No.: HY-17506CAS No.: 83905-01-5Synonyms: CP 62993分式: CHNO分量: 748.98作靶點: Bacterial; Autophagy作通路: Anti-infection; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 1

2、00 mg/mL (133.51 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.34 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic3. 請依序添加每種溶劑： 10% DMSO 90% c

3、orn oilSolubility: 2.5 mg/mL (3.34 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Azithromycin種環內酯抗素，常于治療細菌感染。體外研究 Azithromycin (2 M) augments rhinovirus-induced IFN expression in primary bronchial epithelial cells fromasthmatics, which is associated with over-expression of RIG-I like receptors and repre

4、ssion of viralreplication. Knockdown of MDA5, but not knockdown of RIG-I, diminishes azithromycin (2 M)-enhancedviral-induced IFN expression in asthmatic primary bronchial epithelial cells 1. Azithromycin specificallyreduces MMP-9 mRNA and protein levels without affecting NF-B in endotoxin-challenge

5、d monocytic THP-1cells 2.體內研究 Azithromycin (50 mg/kg) has no effect on bronchoalveolar lavage inflammatory parameters and LDH levels ina mouse model of asthma exacerbation. Azithromycin induces neither general inflammatory parameters norLDH release in a mouse model of asthma exacerbation, and augmen

6、ts expression of interferon-stimulatedgenes and the pattern recognition receptor MDA5 but not RIG-I in exacerbating mice 1.PROTOCOLCell Assay 2 THP-1 cells (106 cells in 1 mL RPMI medium, without antibiotics, growth factors or serum) are seeded ineach well of 24-well plates and allowed to settle for

7、 1 hour. Next, 50 L of the test compound is addedfollowed by 50 L of LPS (final concentration of 10 g/mL). After 24h (37C and 5% CO2) the supernatantsand cell pellets are collected (1200 rpm, 5 min). THP-1 cell viability is tested using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (M

8、TT). MTT is dissolved at 2 mg/mL in PBS and aliquots are stored at -20C. The MTT assay is performed according to the suppliers instructions. Absorbance of MTT convertedinto formazan is measured at a wavelength of 570 nm with background subtraction at 630 nm.MCE has not independently confirmed the ac

9、curacy of these methods. They are for reference only.REFERENCES1. Menzel M, et al. Azithromycin augments rhinovirus-induced IFN via cytosolic MDA5 in experimental models of asthma exacerbation.Oncotarget. 2017 Mar 18.2. Vandooren J, et al. Differential inhibition of activity, activation and gene expression of MMP-9 in THP-1 cells by azithromycin andminocycline versus bortezomib: A comparative study. PLoS One. 2017 Apr 3;12(4):e0174853.McePdfHeightCaution: Product has not been fully validated fo