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  • DC Chemicals Limited
  • China
  • Product Name: Enflicoxib
  • Price: $Inquiry/100mg ¥Inquiry/250mg ¥Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 1 Day
  • Contact: Tony Cao

251442-94-1

251442-94-1 structure
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
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