根皮苷作用機制 - Medchemexpress - MCE中國

1、Product Data SheetPhlorizinCat. No.: HY-N0143CAS No.: 60-81-1分式: CHO分量: 436.41作靶點: SGLT; Na+/K+ ATPase作通路: Membrane Transporter/Ion Channel儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (114.57 mM)H2O : 1 mg/mL (2.29 mM; Need ultrasonic)* means solubl

2、e, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 2.2914 mL 11.4571 mL 22.9142 mL5 mM 0.4583 mL 2.2914 mL 4.5828 mL10 mM 0.2291 mL 1.1457 mL 2.2914 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；旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在

3、1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.73 mM); Clear solution此案可獲得 2.5 mg/mL

4、 (5.73 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.73 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (5.73 mM，飽和度未知) 的澄清溶液。以 1 mL

5、 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.73 mM); Clear solution此案可獲得 2.5 mg/mL (5.73 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Phlorizin種

6、選擇性的 SGLT 抑制劑，對于 hSGLT1 和 hSGLT2 的 Ki 值分別為 300 和 39 nM。Phlorizin 也 個Na+/K+-ATPase 抑制劑。IC & Target Ki: 300 nM (hSGLT1), 39 nM (hSGLT2)1Na+/K+-ATPase2體外研究 Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively1. Phlorizinis also a Na+/K+-ATPase inhibi

7、tor2. Phlorizin at 210-4 M inhibits Na+ and Rb+-activated ATPase activities in humanred cell membranes by 43 %. At 1 mM and 7 mM RbCl, rubidium uptake is not changed or is slightly inhibited (lessthan 15 %) by 210-4 M Phlorizin2. Cell viability is not significantly altered by doses of Phlorizin 100

8、M.Pretreating cells with Phlorizin does not significantly reduce nitrite or PGE2 levels. Phlorizin does not suppress IL-6 orTNF- production, although 100 M Phlorizin can significantly inhibit TNF- expression3.體內(nèi)研究 Prior to Phlorizin treatment, the blood glucose level in SDT fatty rats is 37049 mg/dL

9、. Six hours after dosing, theblood glucose level in the Phlorizin treated group decreases to an almost normal level (13932 mg/dL). Phlorizin- treated SDT fatty rats are heavier than vehicle-treated SDT fatty rats after 12 weeks. Phlorizin treatment significantlydecreases glucose excretion and delays

10、 insulin decreases. Creatinine clearance decreases significantly with Phlorizintreatment. 23 weeks of Phlorizin treatment prevents the decrease of nerve fibers (23.63.2 fibers/mm). Retinalabnormalities are completely prevented with Phlorizin4.PROTOCOLKinase Assay 1 Resealed ghosts are obtained with

11、the addition of 410-3 M ATP and 510-3 M MgCl2 with or without 510-4 MPhlorizin (final concentration) when red cells are hemolyzed. Ghosts corresponding to 0.4-0.45 mL of the originalblood cells are incubated with 0.9 mL of Medium A and 86RbCl for 45 or 90 min and the radioactivity in 200 L of thesup

12、ernatant is determined. The ATPase activity in the resealed ghosts is determined from the increase in inorganicphosphate after incubation1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 3 The RAW264.7 murine macrophage-derived cell line is u

13、sed. Cell viability is measured using the 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cells (105 cells/well) are cultured in 96-wellplates and treated with varying concentrations of Phlorizin for 24 h. Next, the supernatant is removed and the cellsare incubated with MTT

14、 (50 mg/mL) for 4 h at 37C. The plates are washed and isopropanol is added to dissolveformazone crystals, then the absorbance values are measured at 570 nm using a microplate reader3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Female SDT fatt

15、y rats are used in this study. At six weeks of age, SDT fatty rats are divided into two groups (n=8); aPage 2 of 3 www.MedChemEAdministration 4 Phlorizin treated group and a vehicle treated group. Age-matched female Sprague-Dawley (SD) rats are used ascontrol animals (n=8). Animals are housed in a c

16、limate-controlled room (temperature 233C, humidity 5515%, 12h lighting cycle) and allowed free access to basal diet and water. Phlorizin is injected subcutaneously once daily (100 mg/kg/day) to animals in the Phlorizin treated group for 23 weeks. Twenty % propylene glycol is administeredto animals i

17、n the vehicle treated group and control SD rats4.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 RSC Adv. 2018 8:8469-8483. Virus Res. 2020 Feb 15:197901.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Pajor

18、AM, et al. Inhibitor binding in the human renal low- and high-affinity Na+/glucose cotransporters. J Pharmacol Exp Ther. 2008 Mar;324(3):985-91.2. Nakagawa A, et al. Localization of the phlorizin site on Na, K-ATPase in red cell membranes. J Biochem. 1977 May;81(5):1511-5.3. Chang WT, et al. Evaluation of the anti-inflammatory effects of phloretin and phlorizin in lipopolysaccharide-stimulated mouse macrophages. FoodChem. 2012 Sep 15;134(2):972-9.4. Katsuda Y, et al. Contribution of hyperglycemia on diabetic complications in obese type 2 diabetic SDT fatty rats