Phlorizin-Floridzin-DataSheet-MedChemExpress

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作靶点: SGLT; Na+/K+ ATPase作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实

2、验 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制备储备液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

3、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 (5.73 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Sma

4、ll Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.73 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.73 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Phlorizin种选择性的 SGLT 抑制剂，对于 hSGLT1 和 hSGLT2 的 Ki 值分别为 300 和 39 nM。Phlorizin也 个 Na+/K+-ATPase 抑制剂。IC50 & Target Ki: 30

5、0 nM (hSGLT1), 39 nM (hSGLT2) 1Na+/K+-ATPase 2体外研究 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.体内研究 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 您边的抑制剂师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.户使本产品发表的科研献

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