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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]. |
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 | - | - |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 895542-09-3 |
分子式 | C29H33NO4 |
分子量 | 459.58 |
SMILES Code | O=C(C1=CC=C(C2=CC=C(OCCO)C(C3=CC=C(N4CCCC4)C(C(C)(C)C)=C3)=C2)C=C1)O |
MDL No. | MFCD30481310 |
别名 | CD5789 |
运输 | 蓝冰 |
InChI Key | MFBCDACCJCDGBA-UHFFFAOYSA-N |
Pubchem ID | 11518241 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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