Diosmetin - Cytochrome P450 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDiosmetinCat. No.: HY-N0125CAS No.: 520-34-3分式: CHO分量: 300.26作靶點(diǎn): Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: 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 : 35 mg/mL (116.57 mM)* means so

2、luble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.3304 mL 16.6522 mL 33.3045 mL5 mM 0.6661 mL 3.3304 mL 6.6609 mL10 mM 0.3330 mL 1.6652 mL 3.3304 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備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Diosmetin抑制CYP1A酶活性的天然類黃酮, 在HepG2細(xì)胞的 IC50值為40 M。IC50

3、 & Target IC50: 40 M (Others, HepG2 cell) 1體外研究Diosmetin inhibits cell proliferation in HepG2 cells in a concentration-dependent manner. Untreated HepG2cells grow well and are observed to have with normal skeletons, whereas cells treated with diosmetin are1/2 Master of Small Molecules 您邊的抑制劑師www.Med

4、ChemEdistorted and a number of them become round and floating 1.體內(nèi)研究 Pretreatment with diosmetin significantly reduces serum levels of amylase and lipase; the histological injury;the secretion of tumor necrosis factor (TNF)-, interleukin (IL)-1, and IL-6; myeloperoxidase (MPO) activity,trypsinogen a

5、ctivation peptide (TAP) level, the expression of inducible nitric oxide synthase (iNOS); and thenuclear factor (NF)-B activation in cerulein-induced acute pancreatitis 2.PROTOCOLCell Assay 1 Diosmetin is dissolved in DMSO which is maintained at a constant concentration in control samples (2%).HepG2

6、cells are maintained in a humidified atmosphere of 5% CO2 at 37C, and cultured in RPMI-1640medium supplemented with 10% (v/v) fetal bovine serum, 100 U/mL penicillin and 100 U/mL streptomycin.HepG2 cell density is adjusted to 2104 cells/100 L, and the cells are seeded into 96-well plates and placedi

7、n an incubator overnight (37C in 5% CO2) to allow for attachment and recovery. MTT analyses areperformed. Briefly, cells are pretreated with 5, 10, 15 and 20 g/mL diosmetin for 24 h. A total of 20 L MTTsolution (5 mg/mL in PBS) solution is transferred to each well to yield a final 120 L/well and to

8、separatewells a total of 10 L CCK8 (5 mg/mL in PBS) is transferred. The plates are incubated for 4 h at 37C in 5%CO2 and the absorbance is recorded at wavelengths of 595 nm and 450 nm, respectively. The half maximalinhibitory concentration (IC50) of diosmetin is calculated 1.MCE has not independentl

9、y confirmed the accuracy of these methods. They are for reference only.Animal Experimental acute pancreatitis is induced in mice by seven intraperitoneal injection of cerulein (50 g/kg) atAdministration 2 hourly intervals. Diosmetin (100 mg/kg) or vehicle is pretreated 2 h before the first cerulein

10、injection. After 6h, 9 h, 12 h of the first cerulein injection, the severity of acute pancreatitis is evaluated biochemically andmorphologically 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liu B, et al. Diosmetin induces apoptosis by

11、upregulating p53 via the TGF- signal pathway in HepG2 hepatoma cells. Mol Med Rep.2016 Jul;14(1):159-64.2. Yu G, et al. Diosmetin ameliorates the severity of cerulein-induced acute pancreatitis in mice by inhibiting the activation of the nuclearfactor-B. Int J Clin Exp Pathol. 2014 Apr 15;7(5):2133-42.McePdfHeightCaution: Product has not