Y134

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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 ERαERβ 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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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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