Acolbifene 是一种选择性雌激素受体拮抗剂,对雌二醇诱导的 ERα 和 ERβ 转录活性的 IC50 分别为 2 nM 和 0.4 nM。 Acolbifene 显示出抗癌特性。
产品描述
Acolbifene is a selective antagonist of estrogen receptors with IC50s of 2 nM and 0.4 nM for estradiol-induced transcriptional activity of ERα and ERβ. Acolbifene shows an anticarcinogenic property.
体外活性
Acolbifene supports the involvement of the clearance-related receptors in its hypocholesterolemic action without affecting pathways of cholesterol synthesis[2]. Acolbifene inhibits estradiol-stimulated cell proliferation in human breast cancer cancer cells including ZR-75-1, MCF-7 and T-47D[4].
体内活性
In female Sprague-Dawley rats, Acolbifene (2.5 mg/kg; gavage) reduces food intake, strongly decreases cholesterolemia and prevents tumor growth. Acolbifene reduces food intake (16%) and weight gain (45%, mainly fat)[2].
Cas No.
182167-02-8
分子式
C29H31NO4
分子量
457.56
别名
EM-652;阿考比芬
储存和溶解度
DMSO:40 mg/mL (87.4 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years