COX-1 Inhibitor; FR122047

Biochem/physiol Actions

Target IC₅₀: 28 nM and 65 µM for human recombinant COX-1 and COX-2

Reversible: no

Primary TargetCOX-1, COX-2

Product does not compete with ATP.

Cell permeable: yes

General description

A cell-permeable trisubstituted thiazole compound that acts as a potent and selective inhibitor of COX-1 (IC₅₀ = 28 nM and 65 µM for human recombinant COX-1 and COX-2, respectively). Displays ~2,300 fold greater selectivity towards inhibition of COX-1 over COX-2. Reported to be orally active and display analgesic, anti-platelet and anti-inflammatory properties.

A potent, cell-permeable, and selective inhibitor of COX-1 (IC₅₀ = 28 nM; human recombinant COX-1). Does not significantly inhibit COX-2 (IC₅₀ = 65 µM, human recombinant COX-2). Reported to be orally active and displays analgesic properties in chemical nociceptive animal models. Also reported to exhibit anti-inflammatory effects and suppress prostaglandin E2 and thromboxane 2 levels in collagen-induced arthritis in rats. Shown to be 100 times more potent than aspirin in inhibiting arachidonic acid- and collagen-induced human and guinea pig platelet aggregation.

Legal Information

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

Other Notes

Ochi, T., and Goto, T. 2002. Br. J. Pharmacol.135, 782.Ochi, T., et al. 2000. Eur. J. Pharmacol.391, 49.Tanaka, A., et al. 1994. J. Med. Chem.37, 1189.Dohi, M., et al. 1993. Eur. J. Pharmacol.243, 179.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Standard Handling (A)