Firocoxib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Firocoxib 是一种选择性非甾体环氧化酶-2 (COX-2) 抑制剂（IC50 为 0.13 μM），具有抗炎作用。

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.

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.

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.

ML 1785713

Chromatin/Epigenetic

COX

COX-2

——

——

189954-96-9

336.4

C17H20O5S

>98% (HPLC)

DMSO:47mg/ml (139.71 Mm)

CC1(C)OC(=O)C(OCC2CC2)=C1C1=CC=C(C=C1)S(C)(=O)=O

——

(-20℃)

With Ice Pack

≥ 2 years