产品说明书

Adapalene

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Chemical Structure| 106685-40-9 同义名 : CD271
CAS号 : 106685-40-9
货号 : A105293
分子式 : C28H28O3
纯度 : 99%
分子量 : 412.52
MDL号 : MFCD03106112
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 9 mg/mL(21.82 mM),配合低频超声,并水浴加热至45℃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:

IP 2% DMSO+water 0.2 mg/mL clear

PO 0.5% CMC-Na 42 mg/mL suspension

生物活性
描述 Adapalene (CD271) is a third-generation synthetic retinoid commonly used in acne research. It functions as a potent agonist of retinoic acid receptors (RAR), demonstrating AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, and RARα, respectively. Additionally, adapalene inhibits the enzymatic activity of glutamate oxaloacetate transaminase 1 (GOT1) in a non-competitive manner and has shown anti-tumor activity in various studies[1].[2].[3].
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
NCT02731105 Acne Vulgaris Phase 4 Completed - Germany ... 展开 >> Universitätsklinikum Carl Gustav Carus; Klinik und Poliklinik für Dermatologie Dresden, Saxony, Germany, 01307 收起 <<
NCT02620813 Acne Vulgaris Phase 4 Recruiting May 2019 United States, California ... 展开 >> Dermatology Research Area Recruiting Davis, California, United States, 95616 Contact: Negar Foolad, MAS    916-734-1509    nfoolad@ucdavis.edu    Contact: Lauren A Hassoun, BS    916-734-6550    lahassoun@ucdavis.edu    Principal Investigator: Raja K Sivamani, MD          UC Davis Department of Dermatology Recruiting Sacramento, California, United States, 95816 Contact: Raja Sivamani, MD       rajasivamani@gmail.com 收起 <<
NCT02442817 Schizophrenia Phase 4 Unknown May 2017 United States, Nevada ... 展开 >> University of Nevada School of Medicine Recruiting Reno, Nevada, United States, 89503 Contact: Brian Kirkpatrick, MD    775-682-8449    bkirkpatrick@medicine.nevada.edu    Principal Investigator: Brian Kirkpatrick, MD 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL

参考文献

[1]Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.

[2]Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.

[3]Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.