生物活性

Azelaic acid is an organic compound produced by the ozonolysis of oleic acid; component of a number of hair and skin conditioners. Azelaic acid is a dicarboxylic acid that exhibits anti-inflammatory activity. It is known for it's anti acne activity in vitro. Azelaic acid directly inhibits kallikrein 5 (KLK5), downregulating expression of KLK5, toll-like receptor 2 (TLR 2), and cathelicidin, and suppresses activity of serine proteases in vitro, in vivo, and in clinical settings. In PUFA-treated fibroblasts, azelaic acid decreases generation of ROS and upregulates expression of antioxidative enzymes, inhibiting cell damage; agonist activity at PPARν is thought to drive these effects. Azelaic acid also inhibits proliferation of melanocytes. This compound displays antiacne and anticancer potential as well, inhibiting the proliferation of cutaneous melanoma due to suppression of mitochondrial oxidoreductive activity and DNA synthesis.

体外研究

体内研究

激酶实验

细胞实验

动物实验

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

参考文献

[1] Stanisław Han,et al. AAPS PharmSciTech. 2014 Feb; 15(1): 111–120. Published online 2013 Oct 29. doi: 10.1208/s12249-013-0038-y.
[2] Finni Wittek,et al. J Exp Bot. 2014 Nov; 65(20): 5919–5931. Published online 2014 Aug 11. doi: 10.1093/jxb/eru331.

体内溶解度

Clinical Trial Information ( data from http://clinicaltrials.gov )

注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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