189954-96-9
189954-96-9 結(jié)構(gòu)式
基本信息
非羅考昔溶液, 100PPM
3-(環(huán)丙基甲氧基)-5,5-二甲基-4-[4-(甲基磺?；?苯基]-2(5H)-呋喃酮
Equixx
Equioxx
Librens
Previcox
FIROCOXIB
ML 1785713
non-rucoxib
Firocoxib-- GMP
TIANFU CHEM---Firocoxib
物理化學(xué)性質(zhì)
常見問題列表
以化合物A為起始原料，與乙酰氧基乙酰氯反應(yīng)生成化合物B；化合物B加入DBU，于80℃至少反應(yīng)18h，得到化合物C；化合物C再在溶劑DMF中，NaH做堿的條件下與環(huán)丙基溴甲烷反應(yīng)生成非羅考昔。反應(yīng)式如下：
|
COX-2 0.13 μM (IC 50 ) |
COX-1 7.5 μM (IC 50 ) |
The COX-1:COX-2 selectivity ratios generally are established by comparing the IC 50 for COX-1 to the IC 50 for COX-2. The IC 80 value more closely resembles the steady-state plasma drug concentration than does the IC 50 value.The selectivity ratio for Firocoxib based on the IC 80 values is 121 (IC 80 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 IC 50 . 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 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.
| 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. |