Geniposide - Amyloid-β Antagonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGeniposideCat. No.: HY-N0009CAS No.: 24512-63-8分式: CHO分量: 388.37作靶点: Amyloid-作通路: Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (257.49 mM; Need ultrasonic)Mas

2、s Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5749 mL 12.8743 mL 25.7486 mL5 mM 0.5150 mL 2.5749 mL 5.1497 mL10 mM 0.2575 mL 1.2874 mL 2.5749 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，并请注意储备液的保存式和期限。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，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百

3、分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.08 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (7.08 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.08 mM); Clear solu

4、tion1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Geniposide从栀花中提取的环烯醚萜甙; 具有多种物活性，例如抗糖尿病，抗氧化，抗增殖和神经保护活性。体外研究 Geniposide exhibits a variety of activities, such as on antithrombosis, anti-inflammation, anti-diabetes, anti-atherosclerosis, antidepression, healing Alzheimers di

5、sease (AD), anti-hypertension, toxicology, anduntoward reaction are summarized 1. Geniposide markedly declines the production of IL-8, IL-1 and MCP-1 in OGD-induced brain microvascular endothelial cells, the expression of P2Y14 receptor is significantlydown-regulated, the phosphorylation of RAF-1, M

6、EK1/2, ERK1/2 are suppressed 2.体内研究 Geniposide (200 and 400 mg/kg) significantly decreases the blood glucose, insulin and TG levels in diabeticmice in a dose-dependent manner. This compound also decreases the expression of GP and G6Pase atmRNA and immunoreactive protein levels, as well as enzyme act

7、ivity 3. Geniposide (20.0, 40.0, or 80mg/kg) significantly reverses the excessive, alcohol-induced elevation in both serum ALT/AST and hepaticLPO levels. Geniposide upregulates the expression of heme oxygenase-1 (HO-1) to attenuate the cellapoptosis induced by 3-morpholinosydnonimine hydrochloride (

8、SIN-1) in primary cultured hippocampalneurons 4. Geniposide inhibits photochemistry-induced thromboembolism model in vivo. Geniposide arevery effective depressants on NF-B by interrupting IB degradation 1.PROTOCOLCell Assay 2 The third passages of brain microvascular endothelial cells (BMECs) are us

9、ed for the experiment. TheBMECs are divided into four groups: (1)normal control group: the normal cultured BMECs without treatment;(2)OGD group: the BMECs injured by OGD according to the above method; (3) geniposide group: the OGD-injured BMECs treated with 33.2 g/mL geniposide for 6 h; (4)PTX group

10、: the OGD-injured BMECsadministrated with 100 ng/mL PTX. PTX, known as an inhibitor of Gi-coupled receptor is used to assess theactivation of P2Y14 receptor induced by OGD in this experiment 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice:

11、 Type 2 diabetic mice, induced by a high-fat diet and streptozotocin injection, are treated with or withoutAdministration 3 geniposide for 2 weeks. Blood glucose levels are monitored by a glucometer. Insulin concentrations areanalyzed by the ELISA method. Total cholesterol (TC) and triglyceride (TG)

12、 levels are measured usingLabassay kits. Activities of hepatic GP and G6Pase are measured by glucose-6-phosphate dehydrogenase-coupled reaction. Real-time RT-PCR and Western blotting are used to determine the mRNA and proteinlevels of both enzymes 3.MCE has not independently confirmed the accuracy o

13、f these methods. They are for reference only.REFERENCES1. Liu H, et al. Fructus Gardenia (Gardenia jasminoides J. Ellis) phytochemistry, pharmacology ofcardiovascular, and safety with theperspective of new drugs development. J Asian Nat Prod Res. 2013;15(1):94-110.2/3 Master of Small Molecules 您边的抑制

14、剂师www.MedChemE2. Li F, et al. Geniposide attenuates inflammatory response by suppressing P2Y14 receptor and downstream ERK1/2 signaling pathway inoxygen and glucose deprivation-induced brain microvascular endothelial cells. J Ethnopharmacol. 2016 Jun 5;185:77-86.3. Wu SY, et al. Effect of geniposide

15、, a hypoglycemic glucoside, on hepatic regulating enzymes in diabetic mice induced by a high-fat dietand streptozotocin. Acta Pharmacol Sin. 2009 Feb;30(2):202-8.4. Wang J, et al. Geniposide protects against acute alcohol-induced liver injury in mice via up-regulating the expression of the mainantioxidant enzymes. Can J Physiol Pharma