Bioactivity | 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]. | ||||||||||||
Invitro | 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[1].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 Cmax (4.59 μg/mL) following oral administration (rat 20 mg/kg)[3].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]. Animal Model: | ||||||||||||
Name | Aceclofenac | ||||||||||||
CAS | 89796-99-6 | ||||||||||||
Formula | C16H13Cl2NO4 | ||||||||||||
Molar Mass | 354.18 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
|
||||||||||||
Reference | [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. |