AGN 194078 |
Catalog No.GC33315 |
AGN 194078은 선택적 RARα입니다. 각각 3 및 112 nM의 Kd 및 EC50을 갖는 작용제.
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Cas No.: 321995-62-4
Sample solution is provided at 25 µL, 10mM.
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.
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