Ginsenoside-Rb1-Gypenoside-III-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGinsenoside Rb1Cat. No.: HY-N0039CAS No.: 41753-43-9Synonyms: Gypenoside III分式: CHO分量: 1109.29作靶点: Na+/K+ ATPase; IRAK; NF-B; Autophagy; Mitophagy作通路: Membrane Transporter/Ion Channel; Immunology/Inflammation; Protein Tyrosine K

2、inase/RTK; NF- B; Autophagy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 (90.15 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.9015 mL 4.5074 mL 9.0148 mL5 mM 0.1803 mL 0.9015 mL 1.8030 mL10 mM 0.0901 mL 0.4507 mL 0.9015 mL

3、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: 2.5 mg/mL (2.25 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90%

4、 (20% SBE-CD in saline)1/4 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (2.25 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (2.25 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ginsenoside Rb1是中药 Panax ginseng 的成分。Ginsenoside 抑制 Na+, K+-ATPase 活性，IC50 为

5、 6.31.0M。Ginsenoside Rb1 也抑制 IRAK-1 激活及 NF-B p65 的磷酸化。IC50 & Target Na+, K+-ATPase IRAK-1 p65 Autophagy6.3 M (IC50)Mitophagy体外研究 Rat brain microsomal Na+, K+-ATPase activity is inhibited significantly and rapidly by Ginsenoside Rb1. TheIC50 of Ginsenoside Rb1 for Na+,K+-ATPase is 6.31.0 M. The inhib

6、ition is enhanced with increasing theconcentration of Ginsenoside Rb1 or decreasing that of Na+ and K+. Kinetic analysis reveals thatGinsenoside is an uncompetitive inhibitor with respect to ATP 1.Ginsenoside Rb1 significantly inhibits theactivation of interleukin-1 receptor-associated kinase-1 (IRA

7、K-1), IKK-, NF-B, and MAP kinases (ERK,JNK, and p-38); however, interaction between LPS and Toll-like receptor-4, IRAK-4 activation and IRAK-2activation are unaffected 2. Ginsenoside Rb1 is an ingredient of a Chinese medicine Panax ginseng.Ginsenoside Rb1 is a major bioactive compound in the regulat

8、ing pregnane X receptor (PXR)/NF-Bsignaling. Ginsenoside Rb1 is the compound with potent anti-inflammatory activity in ginseng saponin extract(GSE). The concentration for Ginsenoside Rb1 (10 M) is optimized from a preliminary study to ensuresufficient anti-inflammatory activity and without apparent

9、cytotoxicity. Ginsenoside Rb1 significantly reducesTNF-induced upregulation of IL-1 and iNOS mRNA levels, and restores the mRNA levels of PXR andCYP3A4 in LS174T cells. TNF- causes a significant reduction in PXR protein levels and increase in the ratioof phosphorylated to total NF-B p65, both of whi

10、ch are significantly abrogated by Ginsenoside Rb1 3.体内研究 Ginsenoside Rb1 at the both doses of 30mg/kg and 60mg/kg significantly attenuates the histological lunginjury. Ginsenoside Rb1 at the dose of 30mg/kg and 60mg/kg both significantly attenuates the histologicalintestine injury 4. Ginsenoside Rb1

11、 (Rb1), an ingredient of a Chinese medicine Panax ginseng, hasbeneficial effects on mesentery microvascular hyperpermeability induced by Lipopolysaccharide (LPS) andthe underlying mechanisms. In some rats, Ginsenoside Rb1 (5 mg/kg per hour) is administrated through theleft jugular vein 30 min after

12、LPS infusion. Ginsenoside Rb1 decreases caveolae number in endothelial cellsof microvessels. Ginsenoside Rb1 ameliorates microvascular hyperpermeability after the onset ofendotoxemia and improves intestinal edema through inhibiting caveolae formation and junction disruption,which is correlated to su

13、ppression of NF-B and Src activation 5.PROTOCOLCell Assay 3 LS174T cells are seeded in cell imaging dish. After overnight incubation, cells are treated with GSE (100 2/4 Master of Small Molecules 您边的抑制剂师www.MedChemE3. Zhang J, et al. Ginsenosides Regulate PXR/NF-B Signaling and Attenuate Dextran Sul

14、fate Sodium-Induced Colitis. Drug MetabDispos. 2015 Aug;43(8):1181-9.4. Jiang Y, et al. Ginsenoside Rb1 Treatment Attenuates Pulmonary Inflammatory Cytokine Release and Tissue Injury following IntestinalIschemia Reperfusion Injury in Mice. Oxid Med Cell Longev. 2015;2015:843721.5. Zhang Y, et al. Ginsenoside Rb1 ameliorates lipopolysaccharide-induced albumin leakage from rat mesenteric venules by intervening inboth trans- and paracellular pathway. Am J Physiol Gastrointest Liver Physiol. 2014 Feb