Trifarotene

产品说明书

Print
Chemical Structure| 895542-09-3 同义名 : CD5789
CAS号 : 895542-09-3
货号 : A298564
分子式 : C29H33NO4
纯度 : 97%
分子量 : 459.577
MDL号 : MFCD30481310
存储条件：

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(543.98 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Trifarotene is a highly potent and selective agonist for RARγ. It demonstrates approximately 65-fold greater selectivity for RARγ, with an EC50 of 7.7 nM, compared to RARα and RARβ, which have EC50 values of 500 nM and 125 nM, respectively[1]. Trifarotene, applied at 3.3 μL over 0.33 cm² for 24 hours, plays a role in keratinization, desquamation, cornification, and cell adhesion within reconstructed human epidermis (RHE). The average EC50 value for Trifarotene on the combined target genes is 0.0048%. When used in a cream concentration ranging from 0.001% to 0.01% at a dosage of 25 mg/mouse, it exhibits dose-dependent comedolytic activity and is completely effective at a concentration of 0.01%, achieving a 98% reduction[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03738800 Lamellar Ichthyosis Phase 2 Not yet recruiting June 4, 2020 -
NCT02189629 Acne Vulgaris Phase 3 Completed - -
NCT02556788 Acne Vulgaris Phase 3 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL
参考文献

[1]Etienne Thoreau, et al. Structure-based design of Trifarotene (CD5789), a potent and selective RARγ agonist for the treatment of acne. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1736-1741.

[2]J Aubert, et al. Nonclinical and human pharmacology of the potent and selective topical retinoic acid receptor-γ agonist trifarotene. Br J Dermatol. 2018 Aug;179(2):442-456.