生物活性分子抑制剂Adapalene(Synonyms: 阿达帕林; CD271)

生物活性分子抑制剂 特异性抑制剂 激动剂 化合物库 重组蛋白 Adapalene (Synonyms: 阿达帕林; CD271) 纯度: ≥98.0%

Adapalene (CD271) 是第三代合成类视黄醇,局部应用于痤疮。Adapalene 是一种有效的 RAR 激动剂,对 RARβRARγRARαAC50 值分别为 2.3 nM、9.3 nM 和 22 nM。Adapalene 还以非竞争性方式抑制 GOT1 的酶活性。Adapalene 具有抗肿瘤活性。

Adapalene(Synonyms: 阿达帕林; CD271)

Adapalene Chemical Structure

CAS No. : 106685-40-9

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生物活性

Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].

IC50 & Target

AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1]

体外研究
(In Vitro)

Adapalene (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively[2].
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene (10-6-10-3 nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50 of 2.5 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929)
Concentration: 1-200 μM
Incubation Time: 24 hours
Result: Inhibited the viability of cancer cells with higher GOT1 protein expression.

Apoptosis Analysis[2]

Cell Line: ES-2 cells[2]
Concentration: 10, 20, 40 μM
Incubation Time: 24 hours
Result: Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP.

Cell Cycle Analysis[3]

Cell Line: LoVo or DLD1 cells
Concentration: 3, 10, 30 μM
Incubation Time: 6, 12, 24 hours
Result: Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner.

体内研究
(In Vivo)

Adapalene (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3]
Dosage: 15, 20, 65, 100 mg/kg
Administration: P.o. daily for 21 days
Result: Significantly reduced tumor weight and volume.

Clinical Trial

分子量

412.52

Formula

C28H28O3

CAS 号

106685-40-9

中文名称

阿达帕林

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (48.48 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4241 mL 12.1206 mL 24.2412 mL
5 mM 0.4848 mL 2.4241 mL 4.8482 mL
10 mM 0.2424 mL 1.2121 mL 2.4241 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2 mg/mL (4.85 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (4.85 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例,取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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