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