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阿达帕林 /Adapalene {[allProObj[0].p_purity_real_show]}

货号:A105293 同义名: CD271

Adapalene is an agonist of RAR-β (Kd = 34 nM), RAR-γ (Kd = 130 nM) and RXR which is used in the treatment of acne.

Adapalene 化学结构 CAS号:106685-40-9
Adapalene 化学结构
CAS号:106685-40-9
Adapalene 3D分子结构
CAS号:106685-40-9
Adapalene 化学结构 CAS号:106685-40-9
Adapalene 3D分子结构 CAS号:106685-40-9
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Adapalene 纯度/质量文件 产品仅供科研

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Adapalene 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].
体内研究

In vivo, adapalene at dosages of 15 to 100 mg/kg administered orally daily for 21 days inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice, highlighting its potential for clinical use in cancer therapy[3].

体外研究

In cell viability assays, adapalene impacts several cancer cell lines, reducing the viability of ES-2, HOV-7, MCF-7, Hela, SW1990, HT1080, and MM-468 cells. The IC50 values range from 10.36 μM for ES-2 cells to 31.47 μM for MM-468 cells over a 24-hour treatment period at concentrations between 1 and 200 μM[2].

In further experiments, adapalene at 10-40 μM induces apoptosis and inhibits the proliferation of ES-2 cells in vitro[2].

Adapalene also affects cell cycle distribution, significantly increasing the G1-phase population in LoVo and DLD1 cells when applied in concentrations ranging from 3 to 30 μM over periods of 6 to 24 hours[3].

Additionally, adapalene demonstrates inhibition of GOT1 activity with an IC50 of 21.79 μM[2].

Otherwise, Adapalene also effectively suppresses the expression of transglutaminase Type I, a plasma membrane-associated enzyme, with an IC50 of 2.5 nM at concentrations from 10-6 -10-3 nM[1].

Adapalene 动物研究

Dose Pregnant rat: 0.1 mg/kg, 1 mg/kg[3] (p.o.)
Administration p.o.

Adapalene 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 <<

Adapalene 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.

Adapalene 实验方案

计算器
存储液制备 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

Adapalene 技术信息

CAS号106685-40-9
分子式C28H28O3
分子量 412.52
别名 CD271
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

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

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