1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPhlorizinCat. No.: HY-N0143CAS No.: 60-81-1Synonyms: Floridzin; NSC 2833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溶解性數據體外實

2、驗 DMSO : 50 mg/mL (114.57 mM)H2O : 1 mg/mL (2.29 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration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請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式

3、和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄清的儲備液可以根據儲存條件，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 (5.73 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Sma

4、ll Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.73 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.73 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Phlorizin種選擇性的 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。IC50 & Target Ki: 30

5、0 nM (hSGLT1), 39 nM (hSGLT2) 1Na+/K+-ATPase 2體外研究 Phlorizin is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2, respectively1. Phlorizin is also a Na+/K+-ATPase inhibitor 2. Phlorizin at 210-4 M inhibits Na+ and Rb+-activatedATPase activities in human red cell membran

6、es by 43 %. At 1 mM and 7 mM RbCl, rubidium uptake is notchanged or is slightly inhibited (less than 15 %) by 210-4 M Phlorizin 2. Cell viability is not significantlyaltered by doses of Phlorizin 2 levels. Phlorizin does not suppress IL-6 or TNF- production, although 100 MPhlorizin can significantly

7、 inhibit TNF- expression 3.體內研究 Prior to Phlorizin treatment, the blood glucose level in SDT fatty rats is 37049 mg/dL. Six hours after dosing,the blood glucose level in the Phlorizin treated group decreases to an almost normal level (13932 mg/dL).Phlorizin-treated SDT fatty rats are heavier than ve

8、hicle-treated SDT fatty rats after 12 weeks. Phlorizintreatment significantly decreases glucose excretion and delays insulin decreases. Creatinine clearancedecreases significantly with Phlorizin treatment. 23 weeks of Phlorizin treatment prevents the decrease ofnerve fibers (23.63.2 fibers/mm). Reti

9、nal abnormalities are completely prevented with Phlorizin 4.PROTOCOLKinase Assay 1 Resealed ghosts are obtained with the addition of 410-3 M ATP and 510-3 M MgCl2 with or without 510-4 M Phlorizin (final concentration) when red cells are hemolyzed. Ghosts corresponding to 0.4-0.45 mL of theoriginal

10、blood cells are incubated with 0.9 mL of Medium A and 86RbCl for 45 or 90 min and the radioactivityin 200 L of the supernatant is determined. The ATPase activity in the resealed ghosts is determined fromthe increase in inorganic phosphate after incubation 1.MCE has not independently confirmed the ac

11、curacy of these methods. They are for reference only.Cell Assay 3 The RAW264.7 murine macrophage-derived cell line is used. 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-well plates and treated

12、 with varying concentrations of Phlorizin for 24 h. Next, the supernatant is removedand the cells are incubated with MTT (50 mg/mL) for 4 h at 37C. The plates are washed and isopropanol isadded to dissolve formazone crystals, then the absorbance values are measured at 570 nm using amicroplate reader

13、 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEAnimal Female SDT fatty rats are used in this study. At six weeks of age, SDT fatty rats are divided into two groupsAdministration 4 (n=8); a Phlorizin t

14、reated group and a vehicle treated group. Age-matched female Sprague-Dawley (SD) ratsare used as control animals (n=8). Animals are housed in a climate-controlled room (temperature 233C,humidity 5515%, 12 h lighting cycle) and allowed free access to basal diet and water. Phlorizin is injectedsubcuta

15、neously once daily (100 mg/kg/day) to animals in the Phlorizin treated group for 23 weeks. Twenty %propylene glycol is administered to animals in the vehicle treated group and control SD rats 4.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發表的科研獻

16、 RSC Adv. 2018 8:8469-8483.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Pajor AM, et al. Inhibitor binding in the human renal low- and high-affinity Na+/glucose cotransporters. J Pharmacol Exp Ther. 2008Mar;324(3):985-91.2. Nakagawa A, et al. Localization of the phlorizin si

17、te 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 mousemacrophages. Food Chem. 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: eff