1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. Arzoxifene

Arzoxifene  (Synonyms: LY353381; SERM III)

目录号: HY-13556
产品使用指南

Arzoxifene (LY353381) 是一种具有口服活性的选择性雌激素受体调节剂,具有类似 raloxifene 的固定环结构。Arzoxifene 对乳腺癌和子宫内膜有较强的抗雌激素作用,副作用小,对骨和脂质的雌激素有同样强的有利作用。

在相同的摩尔浓度下,化合物盐形式与游离形式有相同的生物活性,但盐形式 Arzoxifene hydrochloride 通常具有更好的水溶性和稳定性。

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Arzoxifene Chemical Structure

Arzoxifene Chemical Structure

CAS No. : 182133-25-1

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Arzoxifene 的其他形式现货产品:

Customer Review

Other Forms of Arzoxifene:

MCE 顾客使用本产品发表的 1 篇科研文献

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

Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator with a fixed ring structure similar to raloxifene. Arzoxifene has minimal side effects with powerful antiestrogenic effects on breast cancer and endometrium, with equally strong favorable estrogenic effects on bone and lipid profile[1].

IC50 & Target

estrogen[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
MCF7 EC50
0.0002 μM
Compound: 8
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
Induction of estrogen receptor-alpha degradation in human MCF7 cells after 4 hrs by in-cell western assay
[PMID: 25879485]
MCF7 IC50
0.3 nM
Compound: 8
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
Antagonist activity at estrogen receptor in human MCF7 cells assessed as inhibition of 17beta-estradiol-mediated transcriptional activation after 24 hrs by luciferase reporter gene assay
[PMID: 25879485]
MCF7 IC50
0.4 μM
Compound: 8
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
Cytotoxicity against human MCF7 cells assessed as cell viability after 5 days by CellTiter-Glo assay
[PMID: 25879485]
体外研究
(In Vitro)

Arzoxifene reduces estrogen receptor expression in endometrial cancer cell lines (ECC-1)[1].

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

体内研究
(In Vivo)

Arzoxifene inhibits MCF-7 breast cancer xenograft growth in oophorectomized athymic mice. Arzoxifene is reported to prevent body weight increase in oophorectomized rats[1].

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

Clinical Trial
分子量

475.60

Formula

C28H29NO4S

CAS 号
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:
Arzoxifene
目录号:
HY-13556
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