Firocoxib

SKU: orb1220099

Description

Firocoxib is a selective non-steroidal inhibitor of cycooxygenase-2 (COX-2) (IC50 of 0.13 μM), with anti-inflammatory for use in dogs and horses.

Key Properties

• CAS Number: 189954-96-9
• MW: 336.4
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₀O₅S
• SMILES: CC1(C)OC(=O)C(OCC2CC2)=C1C1=CC=C(C=C1)S(C)(=O)=O
• Target: COX
• Solubility: DMSO:47mg/ml (139.71 Mm)

Bioactivity

• In Vivo:
  Firocoxib (0.75-1.5 mg/kg; oral gavage; female domestic shorthair cats) treatment efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge. Pharmacokinetic properties ofFirocoxib are determined after i. v. (2 mg/kg) and oral (3 mg/kg) administration in male cats. Firocoxib has moderate to high oral bioavailability (54% to 70%), low plasma clearance (4.7 to 5.8 mL/min/kg), and an elimination half-life of 8.7 to 12.2 hours. Animal model: 14 healthy female domestic shorthair cats (11-15 months old, 2.9-3.9 kg)with lipopolysaccharide (LPS). Dosage: 0.75 mg/kg, 1.5 mg/kg. Administration: Oral gavage. Result: Was efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge.
• In Vitro:
  The COX-1: COX-2 selectivity ratios generally are established by comparing the IC50 for COX-1 to the IC50 for COX-2. The IC80 value more closely resembles the steady-state plasma drug concentration than does the IC50 value. The selectivity ratio for Firocoxib based on the IC80 values is 121 (IC80 of0.36 μM and 43.6 μM for COX-2 and COX-1, respectively), indicating that selectivity for COX-2 is not reduced at concentrations higher than the IC50. Notably, Firocoxib concentrations that yield 80% to 95% inhibition of COX-2 produce < 20% inhibition of COX-1.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ML 1785713

Quick Database Links

Gene Symbol

COX