G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM. Competitive binding studies in endoplasmic reticulum α- (ERα-) and ERβ-expressing cells yielded Ki values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial binding of G-1 at 1 μM.{14210} The discovery of G-1, a compound that does not bind classical ERs, should facilitate further physiological experiments to define the role of GPR30 in vivo.
Size
1 mg
Concentration
n/a
Applications
n/a
Other Names
GPR30 estrogen receptors ER ER.alpha. ER ER.beta. 17b-estradiol 17.beta.-estradiol 17beta-estradiol protein-coupled ERalpha ERbeta endoplasmic reticulum signaling agonists in vivo endocrinology