Y134

立即咨询

Y134

本产品不向个人销售，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。

CAS NO:

849662-80-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

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 (K_i=0.09 nM) 的选择性比对 ERβ (K_i=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。

生物活性

Y134 is a selective and orally activeoestrogen receptor (ER)modulator (SERM), exhibits potent antagonist activity atERαandERβ. Y134 shows 121.1-fold selectivity forERα(K_i=0.09 nM) overERβ(K_i=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breastcancercells^[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].

~~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 E₂in a dose-dependent manner^[1].

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.