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182507-22-8

中文名稱 雷洛昔芬-4' -葡萄糖醛酸苷
CAS 182507-22-8
分子式 C34H35NO10S
分子量 649.71
MOL 文件 182507-22-8.mol
182507-22-8 結(jié)構(gòu)式 182507-22-8 結(jié)構(gòu)式

基本信息

中文別名
雷洛昔芬-4'-葡糖苷酸
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
英文別名
RALOXIFENE-4-GLUCURONIDE
Raloxifene 4'-D-glucuronide
RALOXIFENE-D4-4'-GLUCURONIDE
Raloxifene-4'-glucuronide lithiuM salt
Raloxifene-4'-D-glucuronide lithium salt
Raloxifene-d4-4'-glucuronide lithiuM salt
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-D-glucopyranosiduronic acid)
4-[6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy-d4]benzoyl]benzo[b]thien-2-yl]phenyl-b-D-glucopyranosiduronic Acid

物理化學(xué)性質(zhì)

熔點(diǎn)209-213°C
儲存條件-20°C冷凍

安全數(shù)據(jù)

海關(guān)編碼29389090

常見問題列表

生物活性
Raloxifene 4'-glucuronide 是 Raloxifene 的主要代謝產(chǎn)物。Raloxifene 4'-glucuronide 的形成主要由 UGT1A10 和 UGT1A8 介導(dǎo),以 IC50 為 370 μM 與 estrogen receptor 結(jié)合。Raloxifene 是選擇性雌激素受體調(diào)節(jié)劑。 Raloxifene 在納摩爾濃度激活 TGFβ3 啟動子為完全激動劑,并抑制含雌激素反應(yīng)元件的卵黃蛋白原啟動子的表達(dá)。
靶點(diǎn)

IC50: 370 μM (Estrogen receptor)

體外研究

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.

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