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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.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $76 | In Stock | |
5 mg | $147 | In Stock | |
1 mL x 10 mM (in DMSO) | $162 | In Stock |
Description | 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. |
Targets&IC50 | ERα:2 nM (IC50, E2-induced transcriptional activity), ERβ:0.4 nM (IC50, E2-induced transcriptional activity) |
In vitro | 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]. |
In vivo | 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]. |
Alias | SCH 57068, EM-652 |
Molecular Weight | 457.56 |
Formula | C29H31NO4 |
Cas No. | 182167-02-8 |
Smiles | CC1=C([C@@H](Oc2cc(O)ccc12)c1ccc(OCCN2CCCCC2)cc1)c1ccc(O)cc1 |
Relative Density. | 1.217 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (87.4 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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