阿达帕林

阿达帕林用途

Adapalene(CD-271; Differin)是合成的维甲酸,为维甲酸受体(RAR)激动剂。

阿达帕林作用

阿达帕林是一种维甲酸类化合物，在体内与体外炎症模型中被证明具有抗炎特性，化学结构稳定，在空气和光照下不易分解。作用机理同维甲酸，可与特异的维甲酸核受体结合，区别在于阿达帕林不与和蛋白结合的细胞质受体相结合。在小鼠建立的动物模型进行的皮肤用药试验中证明，阿达帕林可治疗粉刺，并对作为寻常痤疮和分化过程也有作用。作用机制是通过使毛囊上发细胞正常分化而减少微小粉刺形成。在体内与体外的标准抗炎分析中．阿达帕林疗效优于维甲酸，它可抑制人类多核白细胞的化学趋化反应，并可通过抑制花生四烯酸经脂氧化反虚转化为炎症介质媒介物来抑制多形核门细咆的代谢，从而缓解由细胞反应介导的炎性反应。适用于治疗以粉刺、丘疹和脓疱为主要表现的寻常型的皮肤痤疮。亦可用于治疗面部、胸和背部的痤疮。

阿达帕林名称

[ CAS 号 ]:
106685-40-9

[ 中文名 ]:
阿达帕林

[ 英文名 ]:
Adapalene

[中文别名 ]:

[英文别名 ]:

Adapalene
CD-271
Adapalenum
Differin
Adapaleno
Adaferin
MFCD03106112
Differine

阿达帕林生物活性

[ 描述 ]:

Adapalene(CD-271; Differin)是合成的维甲酸,为维甲酸受体(RAR)激动剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> RAR/RXR

研究领域 >> 炎症/免疫

[参考文献]

[1]. Ellis CN, et al. Comparison of adapalene 0.1% solution and tretinoin 0.025% gel in the topical treatment of acne vulgaris. Br J Dermatol. 1998 Oct;139 Suppl 52:41-7.

[2]. Akdeniz N, et al. Anti-inflammatory effects of tretinoin (all-trans-retinoic acid) 0.1% and adapalene 0.1% in rats. Clin Exp Dermatol. 2005 Sep;30(5):570-2.

[相关活性小分子]

维生素A酸；视黄酸 | 4-[(5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基)甲酰氨基]苯甲酸 | 他米巴罗汀 | 4-[(1E)-2-[5,6,7,8-四氢-5,5,8,8-四甲基-3-(1H-吡唑-1-基甲基)-2-萘基]乙烯基]苯甲酸 | 芬维A胺 | 芳维甲酸 | 厚朴酚 | AGN 194310 | AGN 193109 | CD 437 | AR7 | 他扎罗汀 | UVI 3003 | (R)-氟比洛芬(Tarenflurbil) | AGN 195183

阿达帕林物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
606.3±55.0 °C at 760 mmHg

[ 熔点 ]:
319-322ºC

[ 分子式 ]:
C₂₈H₂₈O₃

[ 分子量 ]:
412.520

[ 闪点 ]:
205.9±25.0 °C

[ 精确质量 ]:
412.203857

[ PSA ]:
46.53000

[ LogP ]:
8.04

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.8 mmHg at 25°C

[ 折射率 ]:
1.655

[ 储存条件 ]:
Store at +4°C

阿达帕林MSDS

详细MSDS(安全技术说明书)

阿达帕林安全信息

[ 危害声明 ]:
H413

[ 危险品运输编码 ]:
NONH for all modes of transport

[ 海关编码 ]:
2918990090

阿达帕林合成路线

详细合成路线

阿达帕林上下游产品

阿达帕林上游产品

阿达帕林下游产品

阿达帕林海关

[ 海关编码 ]: 2918990090

[ 中文概述 ]:
2918990090. 其他含其他附加含氧基羧酸（包括酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2918990090. other carboxylic acids with additional oxygen function and their anhydrides, halides, peroxides and peroxyacids; their halogenated, sulphonated, nitrated or nitrosated derivatives. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

阿达帕林文献

Comparison of rheological properties, follicular penetration, drug release, and permeation behavior of a novel topical drug delivery system and a conventional cream.

Eur. J. Pharm. Biopharm. 88(3) , 614-24, (2015)

A novel adapalene-loaded solid lipid microparticle (SLMA) dispersion as a topical drug delivery system (TDDS) for follicular penetration has been introduced. The objective of the present study was to ...

Impaired aldehyde dehydrogenase 1 subfamily member 2A-dependent retinoic acid signaling is related with a mesenchymal-like phenotype and an unfavorable prognosis of head and neck squamous cell carcinoma.

Mol. Cancer 14(1) , 204, (2015)

An inverse correlation between expression of the aldehyde dehydrogenase 1 subfamily A2 (ALDH1A2) and gene promoter methylation has been identified as a common feature of oropharyngeal squamous cell ca...

Origins of the breast milk-derived cells; an endeavor to find the cell sources.

Cell Biol. Int. 39(5) , 611-8, (2015)

Fresh human breast milk consists of a heterogeneous population of cells that may offer a non-invasive source of cells for therapeutic proposes. The aims of this study were to characterize the breast m...

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