349254

NS-398

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

• Synonym(s): NS-398, N-(2-Cyclohexyloxy-4-nitrophenyl)methanesulfonamide
• Empirical Formula (Hill Notation): C₁₃H₁₈N₂O₅S
• CAS Number: 123653-11-2
• Molecular Weight: 314.36
• MDL number: MFCD00882995
• UNSPSC Code: 41121800
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (TLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze
• color: pale yellow
• solubility: DMSO: 20 mg/mL
• shipped in: ambient
• storage temp.: 10-30°C
• SMILES string: [S](=O)(=O)(Nc1c(cc(cc1)[N+](=O)[O-])OC2CCCCC2)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
• InChI key: KTDZCOWXCWUPEO-UHFFFAOYSA-N

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
COX-2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 3.8 µM against COX-2

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Other Notes

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.

Legal Information

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable