楊梅酮作用機制 - Medchemexpress - MCE中國.docx 免費下載
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1、Product Data SheetMyricetinCat. No.: HY-15097CAS No.: 529-44-2分式: CHO分量: 318.24作靶點: Apoptosis; Autophagy; Endogenous Metabolite作通路: Apoptosis; Autophagy; 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)體外實驗 DMSO : 31 mg/mL (97.41 mM)* means soluble
2、, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.1423 mL 15.7114 mL 31.4228 mL5 mM 0.6285 mL 3.1423 mL 6.2846 mL10 mM 0.3142 mL 1.5711 mL 3.1423 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;旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限:-80C, 6 months; -20C, 1 month。-80C 儲存時,請在 6 個內(nèi)使,-20C 儲存時,請在 1
3、 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液,再依次添加助溶劑:為保證實驗結(jié)果的可靠性,澄 的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的作液,建議您現(xiàn)現(xiàn)配,當天使; 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.86 mM); Clear solution此案可獲得 2.5 mg/mL
4、(7.86 mM,飽和度未知) 的澄清溶液。以 1 mL 作液為例,取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中,混合均勻;向上述體系中加50 L Tween-80,混合均勻;然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.86 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (7.86 mM,飽和度未知) 的澄清溶液。以 1 mL
5、作液為例,取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中,混合均勻。BIOLOGICAL ACTIVITY物活性 Myricetin常見的植物來 的類 酮,具有泛的活性,包括強抗氧化,抗癌,抗糖尿病和抗炎活性。IC & Target Human Endogenous Metabolite(批量添加)體外研究 Myricetin exhibits the scavenging activity towards a number of radicals and ions. It displays poor activity (IC
6、50value=1.4 mg/mL) in a superoxide dismutase (SOD)-like activity assay1. It prevents cancer cell death via apoptosisvia regulation of PI3K/Akt and MAPK signalling pathways2. Myricetin exhibits antiphotoaging effects by quenchingcausative free radicals in the skin. Myricetin is able to suppress UVB-i
7、nduced COX-2 expression in mouse skinepidermal JB6 P+ cells. It inhibits UVB-induced initiation of activator protein-1 and NF-, as well as Fyn kinaseactivity1. Myricetin inhibits viability of SKOV3 ovarian cancer cells in a dose-dependent manner. It induces DNA DSBsand ER stress, which leads to apop
8、tosis in SKOV3 cells3. Myricetin inhibits human Hsp70 by more than 80% with IC50values of 83, 11 and 12 M, respectively4.體內(nèi)研究 Treatment of orthotopic pancreatic tumors with myricetin results in tumor regression and decreases metastaticspread2. Exposure to 150 M myricetin causes 14%, 26%, 5% and 49%
9、inhibition of rabbit platelet aggregation,induced by ADP, arachidonic acid, collagen and PAF, respectively5.PROTOCOLCell Assay 2 Pancreatic cancer cells (MIA PaCa-2, Panc-1 or S2-013) or normal pancreatic ductal cells (PDCs) are treated withmyricetin (12.5200 M). Cell viability is determined using t
10、he Dojindo Cell Counting Kit-8. Cells are seeded onto a96-well plate at 1104 cells per well and allowed to adhere overnight. After treatment with myricetin at variousconcentrations for 24 hours, 10 L of the tetrazolium substrate is added to each well of the plate. Plates areincubated at 37C for 1 ho
11、ur, after which the absorbance at 450 nm is measured2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: Mice are given daily intraperitoneal injections of myricetin (30mg/kg in the MIA PaCa-2 model and 50mg/kg inAdministration 2 the S2-013 mo
12、del) or vehicle (DMSO) for 35 days (MIA PaCa-2 model) or 18 days (S2-013 model). Ultrasoundmeasurements are performed at regular intervals to monitor tumor growth. At the end of the in vivo experiment,tumor size is measured using calipers and tumor volume is calculated2.MCE has not independently con
13、firmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Eur J Med Chem. 2019 Dec. Int Immunopharmacol. 2019 Jul 17;75:105742. Biochem Biophys Res Commun. 2018 Sep 3;503(1):297-303.Page 2 of 3 www.MedChemE bioRxiv. 2020 Apr.See more customer validations on HYPERLINK www.MedChemE
14、 www.MedChemEREFERENCES1. Semwal DK, et al. Myricetin: A Dietary Molecule with Diverse Biological Activities. Nutrients. 2016 Feb 16;8(2):90.2. Phillips PA, et al. Myricetin induces pancreatic cancer cell death via the induction of apoptosis and inhibition of thephosphatidylinositol 3-kinase (PI3K)s
15、ignaling pathway. Cancer Lett. 2011 Sep 28;308(2):181-8.3. Xu Y, et al. Myricetin induces apoptosis via endoplasmic reticulum stress and DNA double-strand breaks in human ovarian cancer cells. Mol Med Rep.2016 Mar;13(3):2094-100.4. Jinwal UK, et al. Chemical Manipulation of Hsp70 ATPase Activity Regulates Tau Stability. J Neurosci. 2009 Sep 30;29(39):12079-88.5. Tzeng SH, et al. Inhibition of platelet aggregation by some flavonoids. Thromb Res. 1991 Oct 1;6
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