tcsc0018425 AGN 194078

AGN 194078 is a selective RARα agonist with a K_d and EC₅₀ of 3 and 112 nM, respectively.

IC50 & Target: Kd: 4 nM (RARα)^[1]


EC50: 140 nM (RARα)^[1]

In Vitro: AGN 194078 is a selective RARα agonist and binds to RARα with very high affinity, having a K_d value of 3 nM, while being unable to bind to RARβ and binding only very weakly (K_d=5600 nM) to RARγ. Furthermore, AGN 194078 maintains full transcriptional activity through RARα, with an EC₅₀ value of 112 nM, but only activated

RARβ and RARγ with about 10% efficacy at the highest dose (1000 nM) tested^[1].