G-1

• CAT Number: I010784
• CAS Number: 881639-98-1
• Molecular Formula: C21H18BrNO3
• Molecular Weight: 412.283
• Purity: ≥95%
• Target: Estrogen/progestogen Receptor
• Solubility: Soluble to 100 mM in DMSO
• Storage: Store at -20°C
• IUPAC Name: 1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]ethanone
• InChI: InChI=1S/C21H18BrNO3/c1-11(24)12-5-6-18-15(7-12)13-3-2-4-14(13)21(23-18)16-8-19-20(9-17(16)22)26-10-25-19/h2-3,5-9,13-14,21,23H,4,10H2,1H3
• InChIKey: VHSVKVWHYFBIFJ-UHFFFAOYSA-N
• SMILES: CC(=O)C1=CC2=C(C=C1)NC(C3C2C=CC3)C4=CC5=C(C=C4Br)OCO5

G-1 (CAT: I010784) is a synthetic compound and a potent agonist of the G-protein-coupled estrogen receptor 1 (GPER). GPER, also known as GPR30, is a membrane receptor that mediates estrogen signaling in various tissues and organs. G-1 specifically activates GPER without binding to other estrogen receptors, such as ERα and ERβ. This selective activation of GPER by G-1 leads to downstream cellular responses involved in hormone regulation, cell proliferation, and other physiological processes. G-1 has been studied for its potential therapeutic applications, particularly in the field of cancer research, where GPER activation may influence tumor growth, metastasis, and hormone-related cancers.

Reference

Bologa, C. G., Revankar, C. M., Young, S. M., Edwards, B. S., Arterburn, J. B., Kiselyov, A. S., … & Prossnitz, E. R. (2006). Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature chemical biology,2(4), 207-212.

Blasko, E., Haskell, C. A., Leung, S., Gualtieri, G., Halks-Miller, M., Mahmoudi, M., … & Horuk, R. (2009). Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis. Journal of neuroimmunology, 214(1), 67-77.

Kumar, R., Balhuizen, A., Amisten, S., Lundquist, I., & Salehi, A. (2011). Insulinotropic and antidiabetic effects of 17β-estradiol and the GPR30 agonist G-1 on human pancreatic islets. Endocrinology, 152(7), 2568-2579.