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  3. Lasofoxifene

Lasofoxifene  (Synonyms: 拉索昔芬; CP-336156)

目录号: HY-A0037
产品使用指南

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。

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Lasofoxifene Chemical Structure

Lasofoxifene Chemical Structure

CAS No. : 180916-16-9

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查看 Estrogen Receptor/ERR 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lasofoxifene (CP-336156) is an orally active and selective estrogen receptor modulator (SERM). Lasofoxifene exhibits an anti-osteoporotic function and also inhibits primary tumor growth and metastases. Lasofoxifene can be used for research of breast cancer and 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Lasofoxifene
目录号:
HY-A0037
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