AGN194078是一个有选择性的RARα激动剂，其Kd和EC50值分别为3和112nM。
CAS：321995-62-4
分子式：C22H23F2NO4
分子量：403.42
纯度：98%
存储：Store at -20°C

Background:

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

AGN 194078 is a selective RARα agonist and binds to RARα with very high affinity, having a Kd value of 3 nM, while being unable to bind to RARβ and binding only very weakly (Kd=5600 nM) to RARγ. Furthermore, AGN 194078 maintains full transcriptional activity through RARα, with an EC50 value of 112 nM, but only activatedRARβ and RARγ with about 10% efficacy at the highest dose (1000 nM) tested[1].

[1]. Beard RL, et al. Synthesis and biological activity of retinoic acid receptor-alpha specific amides. Bioorg Med Chem Lett. 2002 Nov 4;12(21):3145-8.