β-Estradiol is an endogenous estrogenic hormone receptor (ER) agonist (Ki values are 0.12 and 0.13 nM for ERα and ERβ respectively). Also high affinity ligand at membrane estrogen GPR30 receptors. β-Estradiol is an activator of PI 3-kinase.
Kuiper et al (1997) Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors a and b. Endocrinology 138 863. Thomas et al (2005) Identity of an estrogen membrane receptor coupled to a G protein in human breast cancer cells. Endocrinology 146 624.
Soluble in DMSO (100 mM), ethanol (75 mM), Dimethylsulfoxide, water (<1 mg/mL), 1:4 solution of DMSO:PBS(pH=7.2) (0.2 mg/mL), DMF, acetone, dioxane, solutions of fixed alkali hydroxides, and vegetable oils (sparingly).
Thank you for your question. We recommend using an organic solvent purged with an inert gas. Solubility in an organic solvent such as ethanol, DMSO or DMF is at least 2.5 mg/ml. This compound is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, the compound should be first dissolved in an organic solvent such as DMSO and then diluted with water. We do not recommend storing in aqueous solutions for more than one day. Great care should be taken to make sure that the organic solvent does not have physiological effects on the experiment.
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IkedaIkeda, M. et al. (PubMed 26384003) investigated wether male and aged female mice would benefit from estrogen administration after cardiac arrest and cardiopulmonary resuscitation (CA/CPR). Post-arrest estrogen administration, using -Estradiol, reduced serum creatinine (sCr) and volume of necrotic tubules (VNT) in young males compared to no affect in young female mice. In aged mice, estrogen significantly reduced sCr and VNT in males and VNT in females. -SCBT Publication Review
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