| Bioactivity | 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[1]. | ||||||||||||
| Invitro | Trifarotene (CD5789) (3.3 µL 0.33 cm2 ; 24 hours) involves in keratinization, desquamation, cornification and cell adhesion in reconstructed human epidermis (RHE). The mean EC50 on the combined target genes is 0.0048% for Trifarotene[2]. | ||||||||||||
| In Vivo | Trifarotene (0.001%-0.01% in a cream at 25 mg/mouse) shows dose-dependent comedolytic activity, being fully efficacious at 0.01% (98% reduction)[2]. Animal Model: | ||||||||||||
| Name | Trifarotene | ||||||||||||
| CAS | 895542-09-3 | ||||||||||||
| Formula | C29H33NO4 | ||||||||||||
| Molar Mass | 459.58 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |