| CAS |
No.60-81-1 |
| 中文名称 |
根皮苷(10mM in DMSO,无菌） |
| 英文名称 |
Phlorizin(10mM in DMSO，Sterile） |
| 分子式 |
C21H24O10 |
| 分子量 |
436.41 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
SGLT |
| 通路 |
Membrane Transporter&Ion Channel |
| 背景说明 |
Phlorizin 是一个 Na+/K+-ATPase 抑制剂，也是一种非选择性的 SGLT 抑制剂。 |
| 生物活性 |
Phlorizin (Floridzin) is a non-selective SGLT inhibitor with Kis of 300 and 39 nM for hSGLT1 and hSGLT2， respectively. Phlorizin is also a Na+/K+-ATPase inhibitor.[1-4] |
| In Vitro |
Phlorizin 是一种非选择性 SGLT 抑制剂，对 hSGLT1 和 hSGLT2 的 Ki 分别为 300 和 39 nM[1]。Phlorizin 也是一种 Na+/K+-ATPase 抑制剂[2]。2×10-4 M 的根皮苷抑制 Na+ 和 Rb+ 激活的人红细胞膜中 43 % 的 ATP 酶活性。在 1 mM 和 7 mM RbCl 下，铷的摄取没有改变或被 2×10-4 M 根皮苷轻微抑制 (小于 15%)[2]。根皮苷 2 水平。根皮苷不抑制 IL-6 或 TNF-α 的产生，但 100 μM 根皮苷可显著抑制 TNF-α 的表达[3]。 |
| In Vivo |
在根皮苷处理之前，SDT 肥胖大鼠的血糖水平为 370±49 mg/dL。给药后 6 小时，根皮苷处理组的血糖水平降至接近正常水平 (139±32 mg/dL)。12 周后，根皮苷处理的 SDT 肥胖大鼠比媒介物处理的 SDT 肥胖大鼠更重。根皮苷处理显著降低葡萄糖排泄并延迟胰岛素降低。根皮苷处理后肌酐清除率显著降低。根皮苷处理 23 周可防止神经纤维减少 (23.6±3.2 纤维/毫米)。Phlorizin[4]可完全预防视网膜异常。 |
| 细胞实验 |
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 with varying concentrations of Phlorizin for 24 h. Next， the supernatant is removed and the cells are incubated with MTT (50 mg/mL) for 4 h at 37°C. The plates are washed and isopropanol is added to dissolve formazone crystals， then the absorbance values are measured at 570 nm using a microplate reader[3]. |
| 动物实验 |
Female SDT fatty rats are used in this study. At six weeks of age， SDT fatty rats are divided into two groups (n=8); a Phlorizin treated group and a vehicle treated group. Age-matched female Sprague-Dawley (SD) rats are used as control animals (n=8). Animals are housed in a climate-controlled room (temperature 23±3°C， humidity 55±15%， 12 h 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 administered to animals in the vehicle treated group and control SD rats[4]. |
| 激酶实验 |
Resealed ghosts are obtained with the addition of 4×10-3 M ATP and 5×10-3 M MgCl2 with or without 5×10-4 M Phlorizin (final concentration) when red cells are hemolyzed. Ghosts corresponding to 0.4-0.45 mL of the original blood cells are incubated with 0.9 mL of Medium A and 86RbCl for 45 or 90 min and the radioactivity in 200 μL of the supernatant is determined. The ATPase activity in the resealed ghosts is determined from the increase in inorganic phosphate after incubation[1]. |
| 数据来源文献 |
[1]. Pajor 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. 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: effects of SGLT inhibitor phlorizin. Exp Anim. 2015;64(2):161-9. |
| 规格 |
1ml |
| 单位 |
瓶 |
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英语
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