LumiraCOXib 是强选择性有口服活性的COX-2抑制剂，Ki值为 0.06?μM。它是非选择性非甾体抗炎试剂，具有抗炎和解热活性，可用于骨关节炎和骨癌研究。

Lumiracoxib is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm (HEK 293 cells transfected with human COX-1). In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1 (COX-1/COX-2 selectivity ratio 515).

Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of Lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis is dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, Lumiracoxib at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac.

Animal Models: Female Lewis ratsFormulation: Sterile phosphate-buffered salineDosages: 0.2–2 mg/kgAdministration: Oral gavage

220991-20-8

C15H13ClFNO2

293.72

Prexige;罗美昔布;COX-189;Lumiracoxib

H2O:<1 mgml
Ethanol:<1 mgml
DMSO:55 mg/mL (187.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years