Firocoxib (ML 1785713) is a potent, selective and orally activeCOX-2inhibitor with anIC₅₀of 0.13 μM. Firocoxib shows 58-fold more selective forCOX-2thanCOX-1(IC₅₀of 7.5 μM). Firocoxib has anti-inflammatory effects^[1].

The COX-1:COX-2 selectivity ratios generally are established by comparing the IC₅₀for COX-1 to the IC₅₀for COX-2. The IC₈₀value more closely resembles the steady-state plasma drug concentration than does the IC₅₀value^[1].
The selectivity ratio for Firocoxib based on the IC₈₀values is 121 (IC₈₀of 0.36 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^[1].

Firocoxib (0.75-1.5mg/kg; oral gavage; female domestic shorthair cats) treatment efficacious in attenuating fever when administered to cats 1 or 14 hours before LPS challenge^[1].
Pharmacokinetic properties of Firocoxib 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^[1].

336.40

Solid

C₁₇H₂₀O₅S

189954-96-9

非罗考昔

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

DMSO : ≥ 52 mg/mL(154.58 mM)

*"≥" means soluble, but saturation unknown.

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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。