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Acolbifene (SCH 57068) 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。
Acolbifene (SCH 57068) 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 629 | 现货 | |
5 mg | ¥ 1,490 | 现货 | |
50 mg | 询价 | 6-8周 | |
1 mL x 10 mM (in DMSO) | ¥ 1,630 | 现货 |
产品描述 | Acolbifene (SCH 57068) 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. |
靶点活性 | ERβ:0.4 nM (IC50, E2-induced transcriptional activity), ERα:2 nM (IC50, E2-induced transcriptional activity) |
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]. |
别名 | 阿考比芬, SCH 57068, EM-652 |
分子量 | 457.56 |
分子式 | C29H31NO4 |
CAS No. | 182167-02-8 |
Smiles | CC1=C([C@@H](Oc2cc(O)ccc12)c1ccc(OCCN2CCCCC2)cc1)c1ccc(O)cc1 |
密度 | 1.217 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 40 mg/mL (87.4 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
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