产品
编 号:F506112
分子式:C29H33NO4
分子量:459.58
产品类型
结构图
CAS No: 895542-09-3
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产品详情
生物活性:
Trifarotene (CD5789) is a potent and selective RARγ agonist. Trifarotene (CD5789) shows ~65-fold and ~16-fold selectivitiy for the RARγ (EC50=7.7 nM) over RARα (EC50=500 nM) and RARβ (EC50=125 nM), respectively.
体内研究:
Trifarotene (乳膏中 0.001%-0.01%,每只小鼠 25 毫克) 显示出剂量依赖性粉刺分解活性,在 0.01% 时完全有效 (减少 98%)。Animal Model:Rhino mice
Dosage:0.001%, 0.0025%, 0.005% and 0.01% in a cream at 25 mg/mouse (5 cm2surface on the back skin on a 5 mg/cm2basis)
Administration:Topical application; once a day; 11 days
Result:Increased the epidermis thickness by 275% (66 μm) and the transepidermal water loss (TEWL) by 285% (26 g/h/m2 ).
体外研究:
Trifarotene (CD5789) (3.3 μL 0.33 cm2 ;24 小时) 参与重建人表皮 (RHE) 的角化、脱屑、角质化和细胞粘附。对于 Trifarotene,联合靶基因的平均 EC50 为 0.0048%。