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Lasofoxifene
本半岛bd体育手机客户端 不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Lasofoxifene图片
CAS NO: 180916-16-9
包装与价格：
包装 价格(元)
100mg 电议
250mg 电议
500mg 电议

半岛bd体育手机客户端 名称
拉索昔芬
CP-336156
半岛bd体育手机客户端 介绍
Lasofoxifene (CP-336156) 是一种具有口服活性和选择性的雌激素受体调节剂 ( SERM)。Lasofoxifene 具有抗骨质疏松的功能，还能抑制原生肿瘤生长和转移。Lasofoxifene 可用于乳腺癌和绝经后骨质疏松症的研究。
生物活性

Lasofoxifene (CP-336156) is an orally active and selectiveestrogen receptormodulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breastcancerand postmenopausal osteoporosis[1][2].
IC50& Target

Target: Estrogen Receptor[1]
体外研究
(In Vitro)

Lasofoxifene (1 nM-1 μM; 48 h) shows antagonist activity on ER+ breast cancer cells without being affected by the expression level of activating ERα mutants relative to wild-type (WT) ERα[2].
体内研究
(In Vivo)

Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) decreases arthritis severity, by reducing cartilage oligomeric matrix protein (COMP), the serum marker of cartilage destruction and reducing serum IL-6 (inflammatory cytokine) levels in mice[1].
Lasofoxifene (4 mg/mice; s.c.; 5 day/week; for 43 d) protects against generalised bone loss in CIA by increasing trabecular bone mineral density (BMD), cortical thickness in mice[1].
Lasofoxifene (5, and 10 mg/kg; s.c.; 5 day/week; for 70 d) exerts function of inhibiting primary tumor growth and reducing metastases to the lung and the liver in mice[3].

Animal Model: Post-menopausal RA model on OVX (ovariectomised) DBA/1 mice (female DBA/1 mice, 8-10 weeks old, CIA-treated)[1]
Dosage: 4 mg/mouse/day
Administration: Subcutaneous injection; 5 days a week from the first signs of arthritis (day 18); 43 days
Result: Reduced in arthritis severity, including synovial inflammation and destruction of joints reduction.
The mean arthritis frequency was 47% while the vehicle group was 81% at 42 days post immunization.
Animal Model: NSG mices with xenograft tumors model (MIND, mammary intraductal): WT, Y537S and D538G ERα render tumors[3]
Dosage: 1, 5, or 10 mg/kg
Administration: Subcutaneous injection; 5 days per week; for 70 days
Result: Elicited a superior inhibitory effect at a dose of 10 mg/kg, resulted potential tumor shrinkage in Y537S and D538G tumors.
And also reduced tumor weight to 60% for Y537S and 50% for D538G at 5 and 10 mg/kg, respectively.
Clinical Trial
分子量

413.55
Formula

C28H31NO2
CAS 号

180916-16-9
中文名称

拉索昔芬
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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