321995-62-4

321995-62-4 structure

Name: AGN 194078
Chemical Name: AGN 194078
CAS Number: 321995-62-4
Molecular Formula: C₂₂H₂₃F₂NO₄
Molecular Weight: 403.42
Catalog: Signaling Pathways Metabolic Enzyme/Protease RAR/RXR
Create Date: 2018-05-25 20:22:24
Modify Date: 2024-01-04 17:29:58
AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.

Name	AGN 194078

Description	AGN 194078 is a selective RARα agonist with a Kd and EC50 of 3 and 112 nM, respectively.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> RAR/RXR Research Areas >> Cancer
Target	RARα:112 nM (EC50) RARα:3 nM (Kd)
In Vitro	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].
References	[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.