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Raloxifene 6-Glucuronide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Raloxifene 6-Glucuronide图片
CAS NO:174264-50-7
包装与价格:
包装价格(元)
1mg电议
5mg电议

产品介绍
Raloxifene 6-glucuronide 是 Raloxifene 的主要代谢产物。Raloxifene 6-glucuronide 的形成主要由 UGT1A1 和 UGT1A8 介导,以IC50为 290 μM 与estrogen receptor结合。 Raloxifene 是选择性非甾体雌激素受体调节剂。Raloxifene 在纳摩尔浓度激活 TGFβ3 启动子为完全激动剂,并抑制含雌激素反应元件的卵黄蛋白原启动子的表达。
生物活性

Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds toestrogen receptorwith anIC50of 290 μM. Raloxifene is a selective and nonsteroidalestrogen receptormodulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].

IC50& Target

IC50: 290 μM (Estrogen receptor)[2]

体外研究
(In Vitro)

Expressed UGT1A8 catalyzes Raloxifene 6-glucuronide with an apparent Kmof 7.9 μM and a Vmaxof 0.61 nmol/min/mg of protein. Based on rates of Raloxifene glucuronidation and known extrahepatic expression, UGT1A8 and 1A10 appear to be primary contributors to Raloxifene glucuronidation in human jejunum microsomes. For human liver microsomes, the variability of Raloxifene 6-glucuronide formation is 3-fold. Correlation analyses reveals that UGT1A1 is responsible for Raloxifene 6-glucuronide but not Raloxifene 4'-glucuronide in liver. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 8-fold for the Raloxifene 6-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 17 μl/min/mg for the Raloxifene 6-glucuronide[2].

分子量

649.71

Formula

C34H35NO10S

CAS 号

174264-50-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.