RXFP3/4 agonist 4 is a potent, selective, nonpeptide dual RXFP3/4 agonist with EC50 of 82/2.0 nM in cellualr cAMP assays.
RXFP3/4 agonist 4 also exhibits GTPγS binding EC50 values 119 nM for RXFP3 and 11 nM for RXFP4.
RXFP3/4 agonist 4 also induces β-arrestin recruitment (EC50=4.9 uM relative to an EC50 of 83 nM for relaxin-3) in an RXFP3 overexpressing U2OS cell line.
RXFP3/4 agonist 4 engages both G protein-mediated cAMP signaling and G protein-independent β-arrestin recruitment, a profile shared by relaxin-3.
