Merck, SML3981-25MG, CITFA

Biochem/physiol Actions
Potent and selective G protein-coupled estrogen receptor (GPER) agonist with significantly higher potency than G-1 and greater selectivity than 17β-estradiol (E2).

CITFA is a potent and selective G protein-coupled estrogen receptor (GPER) agonist that specifically inudces calcium mobilizaton in GPER-transfected, but not non-transfected, COS cells. CITFA is more potent than G-1 (Ca2+ EC50 = 38.7 nM vs. 1.71 μM in HL-60 cells) and, unlike 17β-estradiol (E2), exhibits no affinity toward ERα/β (Ki >10 μM). CITFA (100 nM for 72h) significantly increases axonal and dendritic growth in rat embryonic (E18) hippocampal neurons.