Y134

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 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.

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 IC50ERα and 2.94?nM for ERβ.Y134 (0.01 nM-10 μM; 6 d) inhibits the oestrogen-stimulated ER-expressing breast cancer cell (MCF-7 and T47D) proliferation.Cell Viability Assay 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.

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

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Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

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849662-80-2

472.6

C28H28N2O3S

>98% (HPLC)

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C(=O)(C1=C(SC=2C1=CC=C(O)C2)C3=CC=C(O)C=C3)C4=CC=C(C=C4)N5CCN(C(C)C)CC5

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(-20℃)

With Ice Pack

≥ 2 years