产品
编 号：F478660
分子式：C28H28N2O3S
分子量：472.6
分子式：C28H28N2O3S
分子量：472.6
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CAS No: 849662-80-2
产品详情
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.
体内研究：
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.
体外研究：
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 IC50Y134 相关抗体:Cell Viability AssayCell 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 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.
体内研究：
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.
体外研究：
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 IC50Y134 相关抗体:Cell Viability AssayCell 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.
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