174264-50-7
174264-50-7 結(jié)構(gòu)式
基本信息
雷洛昔芬-6-葡萄糖醛酸苷
雷洛昔芬-6-葡萄糖醛酸苷鋰鹽
雷洛昔芬-D4-6-葡萄糖醛酸苷
Ralaxifene6'-glucuronide
Raloxifene 6'-D-glucuronide
RALOXIFENE-D4-6'-GLUCURONIDE
Raloxifene-6'-glucuronide lithiuM salt
Raloxifene-6-D-glucuronide lithium salt
Raloxifene-d4-6'-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]-D-glucopyranosiduronic acid)
常見問題列表
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.