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. 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.
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- UPC:
- 41105318
- HazmatClass:
- Yes
- WeightUOM:
- LB
- MPN:
- 10008933-10
- CAS:
- 881639-98-1
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