DuP-697, an anti-inflammatory agent, is an inhibitor of Cox-1 and Cox-2 with 50 fold more selectivity for Cox-2 (IC₅₀ of 10 nM) than for Cox-1 (IC₅₀ of 800 nM). DuP-697 has also demonstrated the ability to reduce the exaggerated release of prostaglandin (PG) E₂ elicited by Bradykinin in hydronephrotic kidney cells. Mechanistic studies suggest that DuP-697 interacts reversibly with PG H Synthase-1 while irreversibly inhibiting PGHS-2. Further research shows that DuP-697 suppresses cell growth and induces apoptosis by cell-cycle arrest and caspase-8 activation.

A thiophene that inhibits Cox-2

≥98%

Store at room temperature

Solid

5-溴-2-(4-氟苯基)-3-(4-甲基磺酰基苯基)噻吩;5-bromo-2-(4-fluorophenyl)-3-(4-methylsulfonylphenyl)thiophene

White to off-white solid

1.51 g/cm³

217.51° C

454.08° C at 760 mmHg

n²⁰_D 1.62

COX-2 : IC₅₀ = 10 nM; COX-1: IC₅₀ = 800 nM

Soluble in DMSO (10 mg/mL), ethanol (5 mg/mL), DMF (~54 mg/mL), and 1:1 DMF: PBS (pH 7.2) (~0.5 mg/mL).

3177