京尼平作用機制 - Medchemexpress - MCE中國

1、Product Data SheetGenipinCat. No.: HY-17389CAS No.: 6902-77-8分式: CHO分量: 226.23作靶點: Autophagy作通路: Autophagy儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (442.03 mM)H2O : 4 mg/mL (17.68 mM; Need ultrasonic)* means soluble, but sa

2、turation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 4.4203 mL 22.1014 mL 44.2028 mL5 mM 0.8841 mL 4.4203 mL 8.8406 mL10 mM 0.4420 mL 2.2101 mL 4.4203 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 (protect from light)。-80C 儲存時，請在 6 個內(nèi)使，

3、-20C 儲存時，請在 1 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 (11.05 mM); Clear solution此案

4、可獲得 2.5 mg/mL (11.05 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 (11.05 mM); Clear solution此案可獲得 2.5 mg/mL (11.05 mM，飽和度未知) 的澄清溶液。Page 1 of 2 ww

5、w.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.05 mM); Clear solution此案可獲得 2.5 mg/mL (11.05 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIV

6、ITY物活性 Genipin種天然溶性交聯(lián)劑。體外研究 Genipin stimulats glucose uptake in a time- and dose-dependent manner. The maximal effect is achieved at 2 h with aconcentration of 10 M. In myotubes, genipin promotes glucose transporter 4 (GLUT4) translocation to the cellsurface, which increases the phosphorylation of i

7、nsulin receptor substrate-1 (IRS-1), AKT, and GSK3. Meanwhile,genipin increases ATP levels, closed KATP channels, and then increases the concentration of calcium in the cytoplasmin C2C12 myotubes. Genipin-stimulated glucose uptake could be blocked by both the PI3-K inhibitor wortmannin andcalcium ch

8、elator EGTA. Moreover, genipin increases the level of reactive oxygen species and ATP in C2C12 myotubes1. Genipin increases mitochondrial membrane potential, which then increases ATP levels and closes KATP channels,thereby stimulating insulin secretion in pancreatic -cells. Genipin activates glucose

9、-excited POMC neurons2.Cytochrome c content increases significantly in the cytosol of genipin-treated FaO cells. Activation of caspase-3 andcaspase-7 is ultimately responsible for genipin-induced apoptotic process in hepatoma cells. ROS level notablyincreases in Hep3B cells treated with 200 M genipi

10、n3.PROTOCOLKinase Assay 3 Briefly, the peptide substrate N-acetyl-Asp-Glu-Val-Asp-nitroanilide (Ac-DEVD-NA) is added to the cell lysates inassay buffer (50 mM HEPES, pH 7.4, 100 mM NaCl, 0.1% CHAPS, 10 mM dithiothreitol, 1 mM EDTA, 10% glycerol) andincubated at 37C. The cleavage of the substrate is

11、monitored at 405 nm.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Epigenetics. 2018;13(3):310-317. Eur J Pharmacol. 2019 Feb 15;845:56-64. Molecules. 2018 Mar 16;23(3). pii: E675. Universidade de So Paulo. 2017-04-17.See more customer vali

12、dations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Ma C, et al. Genipin stimulates glucose transport in C2C12 myotubes via IRS-1 and calcium- dependent mechanism. J Endocrinol. 2012 Dec 20.Page 2 of 3 www.MedChemE2. Parton LE, et al. Glucose sensing by POMC neurons regulates glucose homeosta

13、sis and is impaired in obesity. Nature. 2007 Sep 13;449(7159):228-32.3. Kim BC, et al. Genipin-induced apoptosis in hepatoma cells is mediated by reactive oxygen species/c-Jun NH2-terminal kinase-dependent activation ofmitochondrial pathway. Biochem Pharmacol. 2005 Nov 1;70(9):1398-407.4. Ye D, et al. Genipin normalizes depression-like behavior induced by prenatal stress through inhibiting DNMT1. Epigenetics. 2018 Mar 9:1-22.McePdfHeightCaution: