AGN 194078 is a selective RARα agonist with a K d and EC 50 of 3 and 112 nM, respectively.
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 EC 50 value of 112 nM, but only activated\nRARβ and RARγ with about 10% efficacy at the highest dose (1000 nM) tested. MCE has not independently confirmed the accuracy of these methods. They are for reference only.