"目录号: HY-14670
Firocoxib(ML 1785713)是COX-2高效选择性抑制剂，IC50值为0.13uM，比对COX-1的抑制效果强58倍。
相关产品
Celecoxib-Indomethacin-Acetaminophen-Paradol-Aspirin-Ibuprofen-NS-398-Rofecoxib-Diclofenac Sodium-Iguratimod-Parecoxib-Sulindac-Etoricoxib-Naproxen-Valdecoxib-
生物活性
Description
Firocoxib(ML 1785713) is a potent and selective cyclooxygenase (COX)-2 inhibitor with IC50 of 0.13 uM, 58 fold sensitivity for COX2 VSCOX1.IC50 value: 0.13 uM [1]Target: COX2 inhibitorin vitro: Blood concentrations resulting in 50% inhibition of COX-1 and COX-2 activity in vitro were 75 +/- 2 microM and 0.13 +/- 0.03 microM, respectively, and selectivity for inhibiting COX-2 relative to COX-1 was 58. Firocoxib had 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]. in vivo: Administration of firocoxib did not cause any adverse effects on GI, or hematological or serum biochemical variables and appears to have been well tolerated by dogs [2]. Firocoxib (0.5 mg/kg) was initially administered i.v. to calves, and following a 14-day washout period, animals received firocoxib orally prior to cautery dehorning. Firocoxib concentrations were determined by liquid chromatography-tandem mass spectrometry [3]. Firocoxib 5 mg/kg was given orally once daily for 180 days to five dogs with clinical signs and histopathological lesions consistent with solar dermatitis/actinic keratosis. On days 0, 50 and 180, the severity of erythema, skin shine, induration and the number of comedones were evaluated by a clinical scoring system [4].
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