349254

NS-398

A cell-permeable selective inhibitor of COX-2 in vitro.

• Synonyme(s) : NS-398, N-(2-Cyclohexyloxy-4-nitrophenyl)methanesulfonamide
• Formule empirique (notation de Hill): C₁₃H₁₈N₂O₅S
• Numéro CAS: 123653-11-2
• Poids moléculaire : 314.36
• Numéro MDL: MFCD00882995
• Code UNSPSC : 41121800
• Nomenclature NACRES : NA.77

Propriétés

• Niveau de qualité: 100
• Pureté: ≥98% (TLC)
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze
• Couleur: pale yellow
• Solubilité: DMSO: 20 mg/mL
• Conditions d'expédition: ambient
• Température de stockage: 10-30°C
• InChI: 1S/C13H18N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h7-9,11,14H,2-6H2,1H3
• Clé InChI: KTDZCOWXCWUPEO-UHFFFAOYSA-N

Description

Description générale

A cell-permeable selective inhibitor of COX-2 in vitro. Inhibits sheep placental COX-2 (IC₅₀ = 3.8 µM) while COX-1 activity is unaffected at concentrations up to 100 µM. Displays potent anti-inflammatory and analgesic activity in vivo in rat at concentrations from 0.3 to 5 mg/kg.

A cell-permeable, selective inhibitor of cyclooxygenase-2 (COX-2) in vitro. Inhibits sheep placenta COX-2 (IC₅₀ = 3.8 µM) while COX-1 activity is completely unaffected at concentrations up to 100 µM. Displays potent anti-inflammatory and analgesic activity in vivo in rat at concentrations of 0.3 to 5 mg/kg. Does not produce any significant gastrointestinal lesions even at single oral doses of 1000 mg/kg. A useful tool to explore the role of COX-2 in physiologic and pathophysiologic processes.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
COX-2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 3.8 µM against COX-2

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Autres remarques

Ouellet, M., and Percival, M.D. 1995. Biochem. J.306, 247.
Futaki, N., et al. 1994. Prostaglandins47, 55.
Arai, I., et al. 1993. Res. Comm. Chem. Pathol. Pharmacol.81, 259.
Futaki, N., et al. 1993. Gen. Pharmacol.24, 105.
Futaki, N., et al. 1993. J. Pharm.Pharmacol.45, 753.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable