Y134

Research use only, not for human use.

Y134 is an estrogen receptor inhibitor that is selective and orally active, exhibiting strong antagonist activity against ERα and Erβ with Ki of 0.09 nM and 11.31 nM, respectively.

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.

——

Endocrinology/Hormones

Estrogen Receptor/ERR

Estrogen Receptor/ERR

——

——

849662-80-2

472.6

C28H28N2O3S

>98% (HPLC)

——

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

——

(-20℃)

With Ice Pack

≥ 2 years