雷洛昔芬-4' -葡萄糖醛酸苷
| 中文名稱 | 雷洛昔芬-4' -葡萄糖醛酸苷 |
|---|---|
| 中文同義詞 | 雷洛昔芬-4' -葡萄糖醛酸苷;雷洛昔芬-4'-葡萄糖醛酸苷鋰鹽;雷洛昔芬-D4-4' -葡萄糖醛酸苷;雷洛昔芬-4'-葡糖苷酸;4-[6-羥基-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[干冰運輸];普伐他汀-[D9]銨鹽;3,4,5-三羥基-6-[4-[6-羥基-3-[4-[2-(1-哌啶基)乙氧基]苯甲?；鵠苯并噻吩-2-基]苯氧基]四氫吡喃-2-羧酸 |
| 英文名稱 | Raloxifene 4'-glucuronide |
| 英文同義詞 | 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號 | 182507-22-8 |
| 分子式 | C34H35NO10S |
| 分子量 | 649.71 |
| EINECS號 | |
| 相關類別 | Isotope Labelled Compounds;Glucuronides;Intermediates & Fine Chemicals;Metabolites & Impurities;Pharmaceuticals;Isotope Labeled Compounds |
| Mol文件 | 182507-22-8.mol |
| 結(jié)構(gòu)式 |  |
雷洛昔芬-4' -葡萄糖醛酸苷 性質(zhì)
| 熔點 | 209-213°C |
|---|---|
| 沸點 | 949.6±65.0 °C(Predicted) |
| 密度 | 1.444±0.06 g/cm3(Predicted) |
| 儲存條件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（少許）、甲醇（少許） |
| 形態(tài) | 固體 |
| 酸度系數(shù)(pKa) | 2.76±0.70(Predicted) |
| 顏色 | 粘黃色 |
| 穩(wěn)定性 | 吸濕性 |
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
| 海關編碼 | 29389090 |
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