(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol

(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol

中文名称(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
中文同义词化合物 T23620
英文名称(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
英文同义词ACOLBIFENE (hydrochloride);(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol;BYQDPIXWTVEVEA-JMAPEOGHSA-N;(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-(2-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol,hydrochloride
CAS号252555-01-4
分子式C29H31NO4
分子量0
EINECS号
相关类别
Mol文件252555-01-4.mol
结构式(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol 结构式

(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol 性质

溶解度二甲基亚砜:180 mg/ml(364.36 mM)
形态固体
颜色白色至黄色

(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol 用途与合成方法

Acolbifene (EM-652) hydrochloride 是 EM800 的活性代谢物,是具有口服活性的纯抗刺激素和选择性的雌激素受体 (ER) 的拮抗剂,其在 T-47D 细胞中的 IC50 值为 0.110 nM。Acolbifene (EM-652) hydrochloride 具有抗癌活性。

Estrogen receptor

0.110 nM (IC 50 )

Acolbifene (ACOL) does not affect pathways of cholesterol synthesis, supporting the involvement of the clearance-related receptors in its hypocholesterolemic action.
Acolbifene (EM-652) shows no agonistic activity on ERα and ERβ transcriptional function and blocks the estradiol (E2)-mediated activation of both ERα and ERβ.
Acolbifene (EM-652) shows the most potent inhibition of estradiol-stimulated cell proliferation in human breast cancer cells (ZR-75-1, MCF-7, T-47D) and is devoid of any intrinsic estrogenic activity.

Acolbifene (ACOL) reduces food intake and strongly decreases cholesterolemia in rats fed a cholesterol-free diet.
Acolbifene (ACOL) reduces food intake (16%) and weight gain (45%, mainly fat) similarly in both dietary cohorts.

Animal Model: Female Sprague-Dawley rats (n = 42) initially weighing 175-200 g.
Dosage: 2.5 mg/kg.
Administration: Oral gavage, once daily for 21 d.
Result: Prevents tumor growth in rats.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-45mg1800元
2024/04/30HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-410mM * 1mLin DMSO1956元

(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol 上下游产品信息

上游原料
"(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol"相关产品信息
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