Rhapontigenin-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERhapontigeninCat. No.: HY-N2229CAS No.: 500-65-2分式: CHO分量: 258.27作靶點: Cytochrome P450作通路: Metabolic Enzyme/Protease儲存式: Please store the product under the recommended conditions inthe COA.BIOLOGICAL ACTIVITY物活性 Rhapontigenin藜蘆醇的

2、天然類似物，具有抗癌，抗氧化劑，抗真和抗活性。 Rhapontigenin強效選擇性細胞素 P450 1A1 抑制劑 (IC50=400 nM)。Rhapontigenin 對 P450 1A1 的選擇性分別P450 1A2 和P450 1B1 的 400 和 23 倍。IC50 & Target CYP1A1400 nM (IC50)體外研究 Rhapontigenin (0-250 M; 24 hours) demonstrates concentration-dependent anti-cancer activity with an IC50115M in HEP G2 cells 1

3、.Rhapontigenin (20 M; 20 hours) pre-treatment decreases TGF- triggeredincreased snail expression in diverse cancer cells 2.Rhapontigenin (0-20 M; 6 hours) inhibits TGF-induced expression of N-cadherin, vimentin, and CA9 in a dose-dependent manner 2.Rhapontigenin inhibitsADP- and collagen-induced pla

4、telet aggregation with IC50 values of 4 and 70 g/ml, respectively3.Rhapontigenin demonstrates a strong inhibitory activity on the 13-hexosaminidase release induced byDNP-BSA, it exhibits IC50 value of 0.03 mM in RBL 2H3 cells 3.Western Blot Analysis 2Cell Line: HeLa, A549,769-P cellsConcentration: 0

5、 M; 2.5 M; 5 M; 10 M; 20 MIncubation Time: 6 hoursResult: Induced ubiquitination and degradation of HIF-1.1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體內研究 Rhapontigenin (intraperitoneal injection; 25mg/kg) shows significant protection from death due to pulmonarythrombosis in mice, those samples

6、 are orally administered 90 min before tail vein injection of epinephrine andcollagen 3.Animal Model: ICR mice 3Dosage: 25mg/kgAdministration: 25mg/kg; intraperitoneal injectionResult: Showed anti-thrombosis activity with 60% protection.REFERENCES1. Roupe KA, et al. Preparative enzymatic synthesis a

7、nd HPLC analysis of rhapontigenin: applications to metabolism, pharmacokineticsand anti-cancer studies.J Pharm Pharm Sci. 2005 Aug 22;8(3):374-86.2. Yeh YH, et al. Rhapontigenin inhibits TGF-mediated epithelialm esenchym al transition via the PI3K/AKT/m TOR pathway and is notassociated with HIF-1 de

8、gradation.Oncol Rep. 2016 May;35(5):2887-95.3. Park EK, et al. Antithrombotic and antiallergic activities of rhaponticin from Rhei Rhizoma are activated by human intestinal bacteria.ArchPharm Res. 2002 Aug;25(4):528-33.McePdfHeightCaution: Product has not been fully validated for medical applications.For