靶点：COX2 通路：Immunology & Inflammation 背景说明：是一种环氧合酶2抑制剂,可用于骨关节炎,类风湿性关节炎和强直性脊柱炎的相关研究。 生物活性：Aceclofenac is an orally active nonsteroidal anti-inflammatory drug (NSAID)， with analgesic and anti-inflammatory properties. Aceclofenac is used for the research of osteoarthritis， ankylosing spondylitis， rheumatoid arthritis[1-2]. In Vitro：Aceclofenac(1-30 μM; 72 hours)significantly decreases interleukin-6 production and fully blocks prostaglandin E2 synthesis by IL-1β- or LPS-stimulated human chondrocytes.Aceclofenac inhibits COX-1 with IC50 values superior to 100 μM，but decreases by 50% COX-2 activity at the concentration of 0.77 μM in the whole blood test[1].Aceclofenac increases the synthesis of interleukin 1 receptor antagonist and decreases the production of nitric oxide in human articular chondrocytes[2]. In Vivo：Aceclofenac exhibits terminal elimination half-life(rat 3.24 h)due to high plasma clearance(rat 1.10 L/h/kg)following intravenous injection(rat 10 mg/kg)[3]. 数据来源文献：[1]. Y Henrotin， et al. In vitro effects of aceclofenac and its metabolites on the production by chondrocytes of inflammatory mediators. Inflamm Res. 2001 Aug;50(8):391-9. [2]. E Maneiro， et al. Aceclofenac increases the synthesis of interleukin 1 receptor antagonist and decreases the production of nitric oxide in human articular chondrocytes. J Rheumatol. 2001 Dec;28(12):2692-9. [3]. E Maneiro， et al. Keumhan Noh， et al. Absolute bioavailability and metabolism of aceclofenac in rats. Arch Pharm Res. 2015 Jan;38(1):68-72.
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