雷洛昔芬-4' -葡萄糖醛酸苷
| 中文名称 | 雷洛昔芬-4' -葡萄糖醛酸苷 |
|---|---|
| 中文同义词 | 雷洛昔芬-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;雷洛昔芬-4'-葡糖苷酸;4-[6-羟基-3-3-[4-[2-(1-哌啶基)乙氧基]苯甲酰基]苯并[b]噻吩-2-基]苯基 β-D-吡喃葡萄糖醛酸;雷洛昔芬-4-葡糖苷酸[干冰运输];普伐他汀-[D9]铵盐;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 |
| 英文名称 | Raloxifene 4'-glucuronide |
| 英文同义词 | RALOXIFENE-D4-4'-GLUCURONIDE;RALOXIFENE-4-GLUCURONIDE;4-[6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]benzoyl]benzo[b]thien-2-yl]phenyl-D-glucopyranosiduronicacid;4-[6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]benzoyl]benzo[b]thien-2-yl]phenyl-b-D-glucopyranosiduronic Acid;4-[6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy-d4]benzoyl]benzo[b]thien-2-yl]phenyl-b-D-glucopyranosiduronic Acid;(4-[6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy-D4]benzoyl]benzo[b]thien-2-yl]phenyl-D-glucopyranosiduronic acid);Raloxifene-4'-D-glucuronide lithium salt;Raloxifene 4'-D-glucuronide |
| CAS号 | 182507-22-8 |
| 分子式 | C34H35NO10S |
| 分子量 | 649.71 |
| EINECS号 | |
| 相关类别 | Isotope Labelled Compounds;Glucuronides;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Isotope Labeled Compounds |
| Mol文件 | 182507-22-8.mol |
| 结构式 |  |
雷洛昔芬-4' -葡萄糖醛酸苷 性质
| 熔点 | 209-213°C |
|---|---|
| 沸点 | 949.6±65.0 °C(Predicted) |
| 密度 | 1.444±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 形态 | 固体 |
| 酸度系数(pKa) | 2.76±0.70(Predicted) |
| 颜色 | 粘黄色 |
| 稳定性 | 吸湿性 |
IC50: 370 μM (Estrogen receptor)
Expressed UGT1A8 catalyzes Raloxifene 4'-glucuronide with an apparent K m of 59 μM and a V max 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.
安全信息
| 海关编码 | 29389090 |
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