Estrogen receptor (ER) antagonist (Ki values are 1 and 3.6 nM at ERα and ERβ respectively). Shows no agonist activity and is devoid of estrogenic activity. Also a high affinity agonist at GPER (GPR30). Down-regulates the ER and impairs nuclear shuttling and dimerization of the receptor. Shows anticancer activity. Active in vivo.
Solubility & Handling
Solubility overview
Soluble in DMSO (100 mM), and in ethanol (50 mM)
Storage instructions
Room temperature
Storage of solutions
Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions
Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important
This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.
Activation of the human estrogen receptor by the antiestrogens ICI 182,780 and tamoxifen in yeast genetic systems: implications for their mechanism of action.
Dudley MW et al (2000) Proc Natl Acad Sci U S A 97(7) : 3696-701.
Understanding purity and quality - a guide for life scientists
