Trifarotene 是一种有效的选择性 RARγ 激动剂,对 RARγ 的选择性是 RARα 和 RARβ 的 65 倍和 16 倍,EC50分别为7.7、500和125 nM。
产品描述
trifarotene is a potent and selective RARγ agonist with 65-fold and 16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM).
体外活性
Administration of trifarotene involves in keratinization, desquamation, cornification and cell adhesion in reconstructed human epidermis (RHE) with the mean EC50 on the combined target genes of 0.0048%[2].
体内活性
In rhino mice, administration of 0.001%-0.01% Trifarotene shows dose-dependent comedolytic activity. Being fully efficacious at 0.01% with reduction of 98%[2].
Cas No.
895542-09-3
分子式
C29H33NO4
分子量
459.586
别名
CD5789;曲法罗汀
储存和溶解度
DMSO:200 mg/ml(435.18 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years