For research use only. Not for therapeutic Use.
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].
E-6132, one of Enflicoxib (E-6087) metabolites, also inhibits COX-2. After single oral administration of 5 mg/kg of 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].
| Catalog Number | I006394 |
| CAS Number | 251442-94-1 |
| Synonyms | 4-[3-(2,4-difluorophenyl)-5-(trifluoromethyl)-3,4-dihydropyrazol-2-yl]benzenesulfonamide |
| Molecular Formula | C16H12F5N3O2S |
| Purity | ≥95% |
| InChI | InChI=1S/C16H12F5N3O2S/c17-9-1-6-12(13(18)7-9)14-8-15(16(19,20)21)23-24(14)10-2-4-11(5-3-10)27(22,25)26/h1-7,14H,8H2,(H2,22,25,26) |
| InChIKey | ZZMJXWXXMAAPLI-UHFFFAOYSA-N |
| SMILES | C1C(N(N=C1C(F)(F)F)C2=CC=C(C=C2)S(=O)(=O)N)C3=C(C=C(C=C3)F)F |
| Reference | [1]. Carlos Pérez-Maseda, et al. Determination of enantiomeric purity of a novel COX-2 anti-inflammatory drug by capillary electrophoresis using single and dual cyclodextrin systems. Electrophoresis. 2003 May;24(9):1416-21. [2]. R F Reinoso, et al. Pharmacokinetics of E-6087, a new anti-inflammatory agent, in rats and dogs. Biopharm Drug Dispos. 2001 Sep;22(6):231-42. |
