Trifarotene|895542-09-3|(曲法罗汀; CD5789)-陌孚医药/Medlife

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Trifarotene (Synonyms: 曲法罗汀; CD5789)

目录号: PL10806 纯度: ≥98%

CAS No. :895542-09-3

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中文名称	Trifarotene
中文别名	4-[3-(3-tert-butyl-4-pyrrolidin-1-ylphenyl)-4-(2-hydroxyethoxy)phenyl]benzoic acid
英文名称	Trifarotene
英文别名	Trifarotene;CD5789;0J8RN2W0HK;4-[3-(3-tert-butyl-4-pyrrolidin-1-ylphenyl)-4-(2-hydroxyethoxy)phenyl]benzoic acid;3''-(tert-butyl)-4'-(2-hydroxyethoxy)-4''-(pyrrolidin-1-yl)-[1,1':3',1''-terphenyl]-4-carboxylic acid;Trifarotene [USAN:INN];Aklief;Aklief (TN);CD 5789;Trifarotene (USAN/INN);GTPL9962;BCP31392;BDBM50457548;DB12808;compound 15b [PMID: 29706423];3''-Tert-butyl-4'-(2-hydroxyeth;3′′-(1,1-Dimethylethyl)-4′-(2-hydroxyethoxy)-4′′-(1-pyrrolidinyl)[1,1′:3′,1′′-terphenyl]-4-carboxylic acid (ACI);3′′-tert-Butyl-4′-(2-hydroxyethoxy)-4′′-(pyrrolidin-1-yl)[1,1′:3′,1′′]terphenyl-4-carboxylic acid
Cas No.	895542-09-3
分子式	C₂₉H₃₃NO₄
分子量	459.58
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Trifarotene (CD5789) 是一种高效、选择性的 RARγ激动剂。Trifarotene (CD5789) 分别对 RARγ (EC₅₀=7.7 nM) 的选择性比 RARα (500 nM) 高 65 倍，比 RARβ (125 nM) 高 16 倍。

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 (EC 50 =7.7 nM) over RARα (EC 50 =500 nM) and RARβ (EC 50 =125 nM), respectively.

性状

Solid

体外研究(In Vitro)

Trifarotene (CD5789) (3.3 μL 0.33 cm; 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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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). has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 250 mg/mL (543.97 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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