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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGinsenoside ReCat. No.: HY-N0044CAS No.: 52286-59-6Synonyms: Ginsenoside B2; Panaxoside Re; Sanchinoside Re分式: CHO分量: 947.15作靶點: Amyloid-; NF-B; JNK作通路: Neuronal Signaling; NF-B; MAPK/ERK Pathway儲存式: Powder -20C 3 years4C 2 year
2、sIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (52.79 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.0558 mL 5.2790 mL 10.5580 mL5 mM 0.2112 mL 1.0558 mL 2.1116 mL10 mM 0.1056 mL 0.5279 mL 1.0558 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
3、保存式和期限。體內實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?,再依次添加助溶?為保證實驗結果的可靠性,體內實驗的作液,建議您現(xiàn)現(xiàn)配,當天使;澄清的儲備液可以根據(jù)儲存條件,適當保存;以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占):1. 請依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.64 mM); Clear solution2. 請依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.
4、5 mg/mL (2.64 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.64 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ginsenoside Re (Ginsenoside B2)種 Panax notoginseng 提取物。Ginsenoside Re 可降低 -淀粉樣蛋(A)。Ginsenoside Re 還通過抑制 JNK 和 NF-
5、B 發(fā)揮抗炎作。IC50 & Target NF-B JNK A1-40 A1-42體外研究 Ginsenoside Re is a well-known traditional Chinese medicine, which decreases the -site amyloid precursorprotein cleaving enzyme 1 (BACE1) mRNA and protein levels and inhibits BACE1 activity in the N2a/APP695cells. Ginsenoside Re also significantly incre
6、ases the PPAR protein and mRNA levels.To preventGinsenoside Re from having a cytotoxic effect on the N2a/APP695 cells, the cell viability is first determinedby the MTT assay. The N2a/WT and N2a/APP695 cells are treated with increasing concentrations ofGinsenoside Re (0-200 M) for 24 h. Ginsenoside R
7、e concentrations under 100 M do not affect the viabilityof the N2a/WT and N2a/APP695 cells, whereas the 150 M Ginsenoside Re concentration markedlydecreases the survival rate of the N2a/WT and N2a/APP695 cells. Incubation with Ginsenoside Re at a 200M concentration for 24 h reduces the viability of
8、the N2a/WT and N2a/APP695 cells by 15.58% and 26.82%,respectively. These data indicate that Ginsenoside Re treatment within the range of 0-100 M for 24 h is safefor the N2a/WT and N2a/APP695 cells (P0.05) 1.體內研究 Ginsenoside Re reduces insulin resistance in 3T3-L1 adipocytes and high-fat diet (HFD) r
9、ats throughinhibition of JNK and NF-B activation 2. Intraperitoneal injection of lipopolysaccharide (LPS) at a dose of20 mg/kg is lethal to mice, and 70% to 80% of the mice die within 60 h. However, pretreatment of the micewith Rg1 or Ginsenoside Re increases their survival rates in a dose-dependent
10、 manner. With the doses ofRg1 or Ginsenoside Re increase from 2.5 to 5 mg/kg, the survival rate is elevated from 60% to 90% (Rg1) orfrom 30% to 40% (Ginsenoside Re). All the mice administered Rg1 at a minimal dose of 10 mg/kg areprotected from death compared to 80% survival of mice treated with an e
11、qual dose of Ginsenoside Re. Toprotect all the mice, 20 mg/kg Ginsenoside Re is needed. To investigate the anti-inflammatory potential ofRg1 and Ginsenoside Re, 1 mg/kg Rg1 or Ginsenoside Re is injected into rats and then challenged theanimals with LPS. The injection procedure itself causes a transi
12、ent stress-induced increase in bodytemperature of 1.2C in each group. Thereafter, LPS-challenged rats without pretreatment develope arobust biphasic fever, with the first peak reaching 1.5C at 2 h and the second peak reaching 1.8C at 4 h.In contrast, the temperature changes for the Rg1-, Ginsenoside
13、 Re-, and TAK-242-treated groups are only0.9, 1.2, and 0.8C at 2 h and 1.3, 1.4, and 1.0C at 4 h, respectively. Pretreatment with Rg1, GinsenosideRe, or TAK-242 significantly attenuates LPS-induced alterations in body temperature 3.PROTOCOLCell Assay 1 To explore the cytotoxic effect of Ginsenoside
14、Re on N2a/APP695 cells, cell proliferation is assessed usingthe MTT assay. The cells are treated with increasing doses of Ginsenoside Re (0, 25, 50, 100, 150, and 2002/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEM) for 24 h. The MTT assay is performed after the treatments. The cells are incubated
15、 for 4 h at 37 C with0.5 mg/mL of MTT dissolved in fresh complete medium. The dark blue formazan crystals are dissolved inDMSO, and the absorbance is measured on a microplate reader using a reference wavelength of 630 nmand a test wavelength of 490 nm. The data are expressed as the mean percentages
16、of viable cells versus thecontrol 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 To examine the prophylactic effect of Rg1 and Ginsenoside Re on LPS-induced lethality, 6- to 8-week-oldBALB/c mice are randomly assigned to
17、 7 groups with 10 mice in each group. The mice are either leftuntreated or subcutaneously injected with 2.5, 5, 10, or 20 mg/kg Rg1, 20 mg/kg Ginsenoside Re, or 5 mg/kgTAK-242 3 times at 30-min intervals and then challenged with LPS (20 mg/kg) 15 min later. To test thetherapeutic effect of Rg1 and G
18、insenoside Re on LPS-induced lethality, BALB/c mice are assigned to 5groups with 10 mice in each group. The mice are injected intraperitoneally (i.p.) with 20 mg/kg LPS. Fifteenminutes later, mice are subcutaneously injected with 10 mg/kg Rg1, 20 mg/kg Ginsenoside Re, or 5 mg/kgTAK-242 3 times at 30
19、-min intervals or left untreated. Survival rates are recorded for 60 h.Rats 3Sprague Dawley rats are intravenously administered saline solution, 1 mg of Rg1/kg body weight (1 mg/kgRg1), 1 mg/kg Ginsenoside Re, or 1 mg/kg TAK-242. Fifteen minutes later, rats are challenged with 2.5 g/kgLPS. Body temp
20、erature is measured before and after drug administration. Anticoagulated blood samples withEDTA are collected for white blood cell (WBC) counts at indicated time points using a ProCyte Dx automaticblood cell analyzer. Additional blood samples are collected at 4 h post-drug injection and used for pre
21、parationof serum to analyze proinflammatory mediators. The proinflammatory cytokine responses are detected byWestern blot assay.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 J Neurosci Res. 2019 Aug 16.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Cao G, et al. Ginsenosi
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