Y 134

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].

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Cancer

ERα:0.09 nM (Ki)

ERβ:11.31 nM (Ki)

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.

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]. 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.

[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.