Lumiracoxib

SKU: orb1300646

Description

Lumiracoxib (Prexige) is a highly selective COX-2 inhibitor, demonstrating potent activity with an IC50 of 0.14 µM and over 500-fold selectivity versus COX-1. This compound has been utilized in research models to investigate inflammation, pain pathways, and cardiovascular effects in both cellular and animal studies.

Research Area

Immunology & Inflammation, Neuroscience

Key Properties

• CAS Number: 220991-20-8
• MW: 293.72
• Purity: 99.77%
• Formula: C₁₅H₁₃ClFNO₂
• SMILES: N(C1=C(CC(O)=O)C=C(C)C=C1)C2=C(Cl)C=CC=C2F
• Target: COX
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:55 mg/mL (187.25 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.81 mM)

Bioactivity

• Target IC50:
  COX-1 (cell-free assay):Ki:3 μM|COX-2 (cell-free assay):Ki:60 nM
• In Vivo:
  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.
• In Vitro:
  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).
• Animal Research:
  Animal Models: Female Lewis ratsFormulation: Sterile phosphate-buffered salineDosages: 0.2–2 mg/kgAdministration: Oral gavage

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Prexige, bone cancer, Cyclooxygenase, COX, COX 189, COX-1, COX189, COX-189, COX-2, Lumiracoxib, Metabolic Syndrome, osteoarthritis, inflammatory, inhibit, Inhibitor, hyperalgesic

Compound Identifiers

PubChem CID

151166