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252555-01-4

中文名稱 (2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
英文名稱 (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 結(jié)構(gòu)式 252555-01-4 結(jié)構(gòu)式

基本信息

中文別名
化合物 T23620
英文別名
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

物理化學(xué)性質(zhì)

溶解度DMSO: 180 mg/mL (364.36 mM)
形態(tài)Solid
顏色White to yellow
(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-45mg1800元
2024/11/08HY-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
2024/11/08HY-16023(2S)-3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidyl)ethoxy]phenyl]-2H-chromen-7-ol
Acolbifene hydrochloride
252555-01-410mg2900元

常見問(wèn)題列表

生物活性
Acolbifene (EM-652) hydrochloride 是 EM800 的活性代謝物,是具有口服活性的純抗刺激素和選擇性的雌激素受體 (ER) 的拮抗劑,其在 T-47D 細(xì)胞中的 IC50 值為 0.110 nM。Acolbifene (EM-652) hydrochloride 具有抗癌活性。
靶點(diǎn)

Estrogen receptor

0.110 nM (IC 50 )

體外研究

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.

體內(nèi)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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