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252555-01-4

中文名称 (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
英文名称 (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
CAS 252555-01-4
分子式 C29H31NO4
MOL 文件 252555-01-4.mol
252555-01-4 结构式 252555-01-4 结构式

基本信息

中文别名
化合物 T23620
英文别名
ACOLBIFENE (hydrochloride)
BYQDPIXWTVEVEA-JMAPEOGHSA-N
(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-piperidin-1-ylethoxy)phenyl]-2H-chromen-7-ol,hydrochloride

物理化学性质

溶解度DMSO: 180 mg/mL (364.36 mM)
形态Solid
颜色White to yellow
(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2024/08/19HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-45mg1800元
2024/08/19HY-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
2024/08/19HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-410mg2900元

常见问题列表

生物活性
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。
靶点

Estrogen receptor

0.110 nM (IC 50 )

体外研究

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.

体内研究

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.
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