京尼平作用机制 - Medchemexpress - MCE中国

1、Product Data SheetGenipinCat. No.: HY-17389CAS No.: 6902-77-8分式: CHO分量: 226.23作靶点: Autophagy作通路: Autophagy储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性数据体外实验 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制备储备液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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，

3、-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.05 mM); Clear solution此案

4、可获得 2.5 mg/mL (11.05 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (11.05 mM); Clear solution此案可获得 2.5 mg/mL (11.05 mM，饱和度未知) 的澄清溶液。Page 1 of 2 ww

5、w.MedChemE以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄均匀。DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (11.05 mM); Clear solution此案可获得 2.5 mg/mL (11.05 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIV

6、ITY物活性 Genipin种天然溶性交联剂。体外研究 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.户使本产品发表的科研献 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: