(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
- CAS号:252555-01-4
- 英文名:(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
- 中文名:(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
- CBNumber:CB61458796
- 分子式:C29H31NO4
- 分子量:0
- MOL File:252555-01-4.mol
- 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性质、用途与生产工艺
- 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。
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靶点
Estrogen receptor
0.110 nM (IC 50 )
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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.
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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.
- 更新日期:2024/11/08
- 产品编号:HY-16023
- 产品名称:(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol Acolbifene hydrochloride
- CAS编号:252555-01-4
- 包装:5mg
- 价格:1800元
- 更新日期:2024/11/08
- 产品编号:HY-16023
- 产品名称:(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol Acolbifene hydrochloride
- CAS编号:252555-01-4
- 包装:10mM * 1mLin DMSO
- 价格:1956元
- 公司名称:TargetMol Chemicals Inc.
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- 公司名称:Aladdin Scientific
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- 公司名称:MedChemExpress
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