trifarotene

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

trifarotene 是一种有效的选择性 RARγ 激动剂，对 RARγ (EC50=7.7 nM) 的选择性分别是 RARα (EC50=500 nM) 和 RARβ (EC50=125 nM) 的 65 倍和 16 倍。

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).(In Vitro):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%.(In Vivo):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%.

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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 ).

CD5789

Metabolic Enzyme/Protease

Retinoid Receptor

threonine dehydrogenase

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895542-09-3

459.586

C29H33NO4

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (543.97 mM)

CC(C)(C)c1cc(ccc1N1CCCC1)-c1cc(ccc1OCCO)-c1ccc(cc1)C(O)=O

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(-20℃)

With Ice Pack

≥ 2 years