Enflicoxib (C09-1130-793)

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 modelsIn VivoE-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 . 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male and female Wistar rats (250 g) 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.Form:SolidIC50& Target:COX-2. Specification: 0.99 Molecular Formula: C16H12F5N3O2S Molecular Weight: 405.34 PubChem CID: 9953093 Isomeric 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