Y134

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Y134 

Y134 是一种选择性和具有口服活性的雌激素受体 (ER) 调节剂 (SERM)，对 ERα 和 ERβ 表现出强效拮抗剂活性。Y134 对 ERα (Ki=0.09 nM) 的选择性比对 ERβ (Ki=11.31 nM) 高 121.1 倍。Y134 抑制雌激素刺激的 ER 阳性人乳腺癌细胞的增殖。

Y134

Y134 Chemical Structure

CAS No. : 849662-80-2

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生物活性

Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells[1].

IC50 & Target[1]

ERα

0.09 nM (Ki)

ERβ

11.31 nM (Ki)

体外研究
(In Vitro)

Y134 exhibits potent antagonist activity at ERs in CV-1 cells cotransfected with plasmids containing ERα or ERβ and oestrogen-response element-driven luciferase, with IC50[1].
Y134 (0.01 nM-10 μM; 6 d) inhibits the oestrogen-stimulated ER-expressing breast cancer cell (MCF-7 and T47D) proliferation[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MCF-7, T47, MDA-MB-231 cells
Concentration: 0.01 nM-10 μM
Incubation Time: 6 days
Result: Suppressed oestrogen-stimulated MCF-7 and T47D cell proliferation.
Showed no effects on MDA-MB-231 cells, except some cytotoxicity was seen at high concentrations.

体内研究
(In Vivo)

Y134 (1-3 mg/kg/day; p.o. for 3 days) abolishes the E2-induced mammary gland terminal end bud (TEB) outgrowth in ovariectomized rats. Y134 inhibits uterine cell proliferation induced by E2 in a dose-dependent manner[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Four-week old female Sprague-Dawley rats were received ovariectomy[1]
Dosage: 1, 3 mg/kg
Administration: P.o. daily for 3 days
Result: Abolished the effect exerted by E2 in a dose-dependent manner.

分子量

472.60

Formula

C28H28N2O3S
CAS 号

849662-80-2
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.
参考文献

  • [1]. Ning M, et, al. Biological activities of a novel selective oestrogen receptor modulator derived from raloxifene (Y134). Br J Pharmacol. 2007 Jan;150(1):19-28.

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