雷洛昔芬-6-葡萄糖醛酸苷
| 中文名称 | 雷洛昔芬-6-葡萄糖醛酸苷 |
|---|---|
| 中文同义词 | 雷洛昔芬-6'-葡糖苷酸;雷洛昔芬-6-葡萄糖醛酸苷;雷洛昔芬-6-葡萄糖醛酸苷锂盐;雷洛昔芬-D4-6-葡萄糖醛酸苷;雷洛昔芬-6'-GLUCURONIDE_D4;雷洛昔芬 D4 6 葡糖苷酸;2-(4-羟基苯基)-3-{4-[2-(1-哌啶基)乙氧基]苯甲酰基}-1-苯并噻吩-6-基(5XI)-BETA-D-来苏-吡喃己酮糖苷酸;雷洛昔芬6-O-Β-D-葡萄糖醛酸苷 |
| 英文名称 | Raloxifene 6'-glucuronide |
| 英文同义词 | Raloxifene-6'-glucuronide lithiuM salt;Raloxifene-d4-6'-glucuronide lithiuM salt;RALOXIFENE 6-GLUCURONIDE;RALOXIFENE-D4-6'-GLUCURONIDE;Raloxifene-6-D-glucuronide lithium salt;2-(4-Hydroxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxybenzoyl]benzo[b]thien-6-yl]-D-glucopyranosiduronicacid;2-(4-Hydroxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxybenzoyl]benzo[b]thien-6-yl]-b-D-glucopyranosiduronic Acid;2-(4-Hydroxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy-d4-benzoyl]benzo[b]thien-6-yl]-b-D-glucopyranosiduronic Acid |
| CAS号 | 174264-50-7 |
| 分子式 | C34H35NO10S |
| 分子量 | 649.71 |
| EINECS号 | |
| 相关类别 | Glucuronides;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Isotope Labeled Compounds;Isotope Labelled Compounds |
| Mol文件 | 174264-50-7.mol |
| 结构式 |  |
雷洛昔芬-6-葡萄糖醛酸苷 性质
| 熔点 | 210-214°C (dec.) |
|---|---|
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（轻微）、甲醇（轻微、加热） |
| 形态 | 固体 |
| 颜色 | 黄色至深黄色 |
IC50: 290 μM (Estrogen receptor)
Expressed UGT1A8 catalyzes Raloxifene 6-glucuronide with an apparent K m of 7.9 μM and a V max of 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.
安全信息
| 海关编码 | 29389090 |
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