| 生物活性 |
Raloxifene 4'-Glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression. |
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| IC50&Target |
IC50: 370 μM (Estrogen receptor) |
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| 体外研究 |
Expressed UGT1A8 catalyzes Raloxifene 4'-glucuronide with an apparent Km of 59 μM and a Vmax of 2.0 nmol/min/mg. 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 4'-glucuronide formation is 4-fold. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 9-fold for the Raloxifene 4'-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 95 μl/min/mg for the Raloxifene 4'-glucuronide. |
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| 分子式 |
C34H35NO10S
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| 分子量 |
649.71
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| CAS号 |
182507-22-8
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| 中文名称 |
3,4,5-三羟基-6-[4-[6-羟基-3-[4-[2-(1-哌啶基)乙氧基]苯甲酰基]苯并噻吩-2-基]苯氧基]四氢吡喃-2-羧酸;雷洛昔芬-4''-葡糖苷酸;雷洛昔芬-4'-葡糖苷酸;雷洛昔芬-4-葡糖苷酸;雷洛昔芬-4'-葡萄糖苷酸;雷洛昔芬4'-葡萄糖醛酸苷标准品;雷洛昔芬-D4-4'葡萄糖醛酸苷;雷洛昔芬-4'-葡萄糖醛酸苷锂盐;雷洛昔芬-D4-4' -葡萄糖醛酸苷
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
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纯度： ≥95%
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