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
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	Research Areas >> Inflammation/Immunology Signaling Pathways >> Immunology/Inflammation >> COX
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	[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.

Molecular Formula	C₁₆H₁₂F₅N₃O₂S
Molecular Weight	405.34
Exact Mass	405.05700
PSA	84.14000
LogP	4.76360

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