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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGinsenoside Rg2Cat. No.: HY-N0602CAS No.: 52286-74-5Synonyms: Chikusetsusaponin I; Panaxoside Rg2; Prosapogenin C2分式: CHO分量: 785.01作靶點(diǎn): NF-B; Amyloid-作通路: NF-B; Neuronal Signaling儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C
2、 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (127.39 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.2739 mL 6.3693 mL 12.7387 mL5 mM 0.2548 mL 1.2739 mL 2.5477 mL10 mM 0.1274 mL 0.6369 mL 1.2739 mL請(qǐng)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(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)
3、您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?,配制前?qǐng)先配制澄清的儲(chǔ)備液,再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性,體內(nèi)實(shí)驗(yàn)的作液,建議您現(xiàn)現(xiàn)配,當(dāng)天使;澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)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(qǐng)依序添加每種溶劑: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.18 mM); Clear solution2. 請(qǐng)依序添加每種溶劑: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.18
4、mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑: 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.18 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ginsenoside Rg2參的主 活性成分之。Ginsenoside Rg2 種 NF-B 抑制劑。 Ginsenoside Rg2 還降低 A1-42 積聚。IC50 & Target NF-B A1-42體外研究 Ginsenoside Rg2
5、prevents the decrease of IB expression stimulated with lipopolysaccharide (LPS). IBdissociation from RelA-p50 complex is crucial for NF-B activity. Ginsenoside Rg2, protopanaxatriol, inhibitsvascular cell adhesion molecule 1 (VCAM-1) and intercellular adhesion molecule 1 (ICAM-1) expressionstimulate
6、d with LPS from human umbilical vein endothelial cell (HUVEC). The inhibition of VCAM-1 andICAM-1 expression by Ginsenoside Rg2 is in a concentration-dependent manner, significantly. Treatment ofendothelial cells with LPS (1g/mL) decreases IB expression. By 1 hr after LPS treatment, significantdecre
7、ase of IB is attained. To determine whether LPS-stimulated IB expression is affected byGinsenoside Rg2, endothelial cells are treated for 1 hr with Ginsenoside Rg2 (150 M) prior to LPS (1g/mL) stimulation for 1 hr. Ginsenoside Rg2 reverses the decrease of LPS-induced IB expression in aconcentration-
8、dependent manner, significantly. The adhesion of THP-1 cells to endothelial cells is measuredusing quantitative monolayer adhesion assay. The adhesion of THP-1 cells onto endothelial cells areincreased to five folds by LPS (1 g/mL) stimulation for 8 hrs. Ginsenoside Rg2 (150 M) inhibits theadhesion
9、of THP-1 cells to endothelial cells stimulated with LPS, in a concentration-dependent manner 1.體內(nèi)研究 G-Rg1 and Ginsenoside Rg2 (G-Rg2) reduce the escape latencies on the last two training days compared tothe Alzheimers disease (AD) model group (p1-42 accumulation in APP/PS1 mice. In the G-Rg1 andGins
10、enoside Rg2 treated mice, the pathological abnormalities observed in the APP/PS1 mice are graduallyameliorated. Clear nucleoli and light brown, sparsely scattered A deposits are visible 2.PROTOCOLCell Assay HUVECs ares grown in EBM-2 containing 10% FBS at a density of 2.0105 cells/well on 24-well pl
11、ates.Endothelial cells at 9095% confluence are treated with Ginsenoside Rg2 (1, 20, 50 M) for 1 hr prior to 1g/mL of LPS stimulation for 8 hr. THP-1 cells are labeled with Calcein-AM (5 M) in RPMI 1640 mediumcontaining 10% FBS for 30 min. After extensive washing with PBS, the labeled THP-1 cells are
12、 seeded at adensity of 5.0105 cells/well onto endothelial cells which are treated with the Rg2 and/or LPS and, then,incubated for 1 hr at 37C while gentle shaking. After incubation, non-adherent cells are removed by gentlewashing two times with PBS. Photograph images are obtained at 485 nm excitatio
13、n and 538 nm emissionusing a SPOT II digital camera-attached fluorescence microscope 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 22/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAdministration 2 Male APP/PS1 mice, weighing 202 g, and
14、male C57BL/6J mice, weighing 202 g, are used. The animalsare maintained in an air-conditioned animal center at 232C and a relative humidity of 5010%, with anatural light-dark cycle. Food and water are available ad libitum. After acclimatization for 1 wk, the mice aredivided into four groups (n=10 in
15、 each group): the normal control group, the AD model group, the G-Rg1group, and the Ginsenoside Rg2 group. According to the concentration-response curves, the mice in the G-Rg1 and Ginsenoside Rg2 groups are injected intraperitoneally once daily with G-Rg1 and Ginsenoside Rg2(30 mg/kg), respectively
16、, dissolved in saline. The mice in the AD model group (APP/PS1 mice) and thenormal control group (C57BL/6J nontransgenic littermates) are treated with isodose saline (0.9% w/v). Allmice are treated for 1 mo before brain metabolite profiling.MCE has not independently confirmed the accuracy of these m
17、ethods. They are for reference only.REFERENCES1. Cho YS, et al. Ginsenoside rg2 inhibits lipopolysaccharide-induced adhesion molecule expression in human umbilical vein endothelialcell. Korean J Physiol Pharmacol. 2013 Apr;17(2):133-7.2. Li N, et al. A UPLC/MS-based metabolomics investigation of the protective effect of ginsenosides Rg1 and Rg2 in mice
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