AGN 194078 is a selective RARα agonist with a K d and EC 50 of 3 and 112 nM, respectively.
性状
Solid
IC50 & Target[1][2]
Kd: 4 nM (RARα)
EC50: 140 nM (RARα)
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (247.88 mM; Need ultrasonic)配制储备液
[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.