产品
编 号:F237454
分子式:C17H20O5S
分子量:336.4
产品类型
结构图
CAS No: 189954-96-9
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产品详情
生物活性:
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.
体内研究:
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.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.
体外研究:
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 Firocoxib 相关抗体: