Diosmin _Aryl Hydrocarbon Receptor Agonist - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDiosminCat. No.: HY-N0178CAS No.: 520-27-4分式: CHO分量: 608.54作靶點(diǎn): Aryl Hydrocarbon Receptor作通路: Immunology/Inflammation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 : 32 mg/mL (52.58 mM; Need

2、 ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6433 mL 8.2164 mL 16.4328 mL5 mM 0.3287 mL 1.6433 mL 3.2866 mL10 mM 0.1643 mL 0.8216 mL 1.6433 mL請(qǐng)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(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Diosmin在各種柑橘類果中發(fā)現(xiàn)的類黃酮，也是芳烴受體 (AhR) 的激動(dòng)劑。IC50 & Target AhR 1體外研究Treatmen

3、t with Diosmin causes a dose dependent increase in the amount of adducts formed (up to a 7-foldincrease in adducts at 5 M Diosmin). At 5 M, Diosmin increases the cytotoxicity of 7,12-dimethylbenz(a)anthracene (DMBA), shifting the IC50 of DMBA from an estimated 1.2 M to 400 nM.1/2 Master of Small Mol

4、ecules 您邊的抑制劑師www.MedChemEDiosmin is not cytotoxic in itself at the concentrations tested. Diosmin causes an increase in CYPIAI activityin MCF-7 cells in a time- and dose-dependent fashion. Diosmin causes a dose-dependent increase inCYPIAI mRNA after 24 h of incubation, causes a long-lasting increas

5、e in CYPIAI mRNA accumulation thatreaches its peak after 48 h of incubation 1.體內(nèi)研究 Diosmin significantly decreases the malondialdehyde (MDA) levels and increases the activities of total-superoxide dismutase (T-SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) in the retina of ratscompare wit

6、h the ischemia group (P 2.PROTOCOLCell Assay 1 MCF-7 cells are plated at 25,000 cells/well in 24-well plates. After 24 h, the medium is changed to mediumcontaining 5 M Diosmin. After an additional 24 h, the medium is again changed with medium containing 5 M Diosmin. After 3 days, the total cell grow

7、th is assessed by sulforhodamine 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Healthy male Wistar rats (n=112) weighing 180 to 200g each are used in this study. The animals areAdministration 2 randomly assigned to the following 4 groups, whi

8、ch include combinations of the ischemia/reperfusion (I/R)injury model or sham injury with the i.g. administration of Diosmin or vehicle solution: sham+vehicle (SV)group, sham+Diosmin (SD) group, model+vehicle (MV) group, and model+Diosmin (MD) group. Forintragastric administration, 5mL of 2% Diosmin

9、 per kilogram weight of the rat, or the same volume of vehiclesolution, is administered intragastrically 30min before the onset of ischemia, and then daily after I/R injuryuntil the animals are sacrificed. Using an overdose of anesthesia, 8 rats from each group are sacrificed 24hafter I/R injury, an

10、d their eyeballs harvested for determination of the malondialdehyde (MDA) level and theactivities of total-superoxide dismutase (T-SOD), glutathione peroxidase (GSH-Px), and catalase (CAT). At 7days post-I/R injury, electroretinograms (ERGs) are recorded in 6 rats per group. Meanwhile, 6 rats in eac

11、hgroup are randomly chosen for retrograde labeling of retinal ganglion cells (RGCs) , and the remaining 8 ratsfrom each group are histopathologically examined 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ciolino HP, et al. Diosmin and diosmetin are agonists of the aryl hydrocarbon receptor that differentially affectcytochrome P450 1A1activity. Cancer Res. 1998 Jul 1;58(13):2754-60.2. Tong N, et al. Diosmin protects rat retina from ischemia/reperfusion injury. J Ocul Pharmacol Ther. 2012 Oct;28(5):459-66.McePdfHeightCaution: Pr