251442-94-1
251442-94-1 structure
- Name: Enflicoxib
- Chemical Name: 1-(4-aminosulphonylphenyl)-5-(2,4-difluorophenyl)-4,5-dihydro-3-trifluoromethyl-1H-pyrazole
- CAS Number: 251442-94-1
- Molecular Formula: C16H12F5N3O2S
- Molecular Weight: 405.34
- Catalog: Signaling Pathways Immunology/Inflammation COX
- Create Date: 2018-04-24 07:03:30
- Modify Date: 2024-01-06 19:05:09
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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].
| Name | 1-(4-aminosulphonylphenyl)-5-(2,4-difluorophenyl)-4,5-dihydro-3-trifluoromethyl-1H-pyrazole |
|---|---|
| Synonyms |
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 |
| 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 |
| Molecular Formula | C16H12F5N3O2S |
|---|---|
| Molecular Weight | 405.34 |
| Exact Mass | 405.05700 |
| PSA | 84.14000 |
| LogP | 4.76360 |