化合物Y134 T23540

Product Introduction
Bioactivity


英文名: Y134

描述: Y134 是一种雌激素受体的抑制剂，具有 选择性和具有口服活性，对 ERα 和 ERβ 表现出强效拮抗剂活性，Ki 分别为 0.09 nM 和11.31 nM。 Y134 对 ERα 的选择性比对 ERβ 高 121.1 倍。 Y134 对雌激素刺激的 ER 阳性人乳腺癌细胞的增殖具有抑制作用。

体外活性: Y134 displays robust antagonistic effects on estrogen receptors (ERs) in CV-1 cells co-transfected with plasmids carrying ERα or ERβ along with estrogen-response element-driven luciferase, resulting in a significant decrease in luciferase activity.[1]Treatment with Y134 (0.01 nM-10 μM; 6 d) effectively suppresses the proliferation of ER-expressing breast cancer cells (MCF-7 and T47D) stimulated by estrogen.[1]

体内活性: Administration of Y134 (1-3 mg/kg/day; p.o. for 3 days) completely eliminates the estrogen-induced growth of terminal end buds (TEB) in the mammary glands of ovariectomized rats. Y134 exhibits a dose-dependent inhibition of uterine cell proliferation induced by estrogen (E2). [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 47.26mg/ml (90.0 mM)
Ethanol : 47.26mg/ml (90.0 mM)


关键字: Y134 | Y-134

相关产品: (-)-(S)-Equol | Saikosaponin D | Bazedoxifene hydrochloride | ER degrader 6 | Estradiol dipropionate | Estropipate | (±)-Equol | Isopsoralenoside | β-Estradiol 17-acetate | Kaempferol

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Nuclear Receptor Compound Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途