Enflicoxib
Names
[ CAS No. ]:
251442-94-1
[ Name ]:
Enflicoxib
[Synonym ]:
1-(4-aminosulphonylphenyl)-5-(2,4-difluorophenyl)-4,5-dihydro-3-trifluoromethyl-1H-pyrazol
(+/-)-1-(4-aminosulphonylphenyl)-5-(2,4-difluorophenyl)-4,5-dihydro-3-trifluoromethyl-1H-pyrazole
Biological Activity
[Description]:
Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models[1].
[Related Catalog]:
[Target]
COX-2
[In Vivo]
"E-6132, one of Enflicoxib (E-6087) metabolites, also inhibits COX-2. After single oral administration of 5 mg/kgof E-6087 to rats, plasma concentrations of Enflicoxib at peak time are higher than those of E-6132, suggesting that activity is mainly due to Enflicoxib[1]. Enflicoxib (E-6087) is characterized by a long elimination half-life (20-35 h), a low plasma clearance (0.10-0.22 L/h/kg) and a relatively large volume of distribution (2-6 L/kg) in rats and dogs after single oral and intravenous doses. Enflicoxib and E-6132 (a pharmacologically active metabolite) show different pharmacokinetics. The higher percentage of Enflicoxib at early times suggests that Enflicoxib is the main compound responsible for in vivo activity, although E-6132 would contribute to the activity at later times[2]." Animal Model: Male and female Wistar rats (250 g)[1] Dosage: 5 mg/kg Administration: Administered by gastric gavage (10 mL/kg); a single oral dose Result: Plasma concentrations of E-6087 at peak time are higher than those of E-6132.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C16H12F5N3O2S
[ Molecular Weight ]:
405.34
[ Exact Mass ]:
405.05700
[ PSA ]:
84.14000
[ LogP ]:
4.76360