Chemical Name |
Firocoxib |
CAS Number |
189954-96-9 |
MDL Number |
MFCD09837800 |
Molecular Formula |
C17H20O5S |
Molecular Weight |
336.40 |
Synonyms |
ML 1785713 |
Introduction of 189954-96-9 :
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1]. 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[1].
The selectivity ratio for Firocoxib based on the IC80 values is 121 (IC80 of 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]. In Vivo: 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].
Purity |
NLT 98% |
Storage |
at 20ºC 2 years |
*The above information is for reference only.