COX-1 Inhibitor, FR122047 - CAS 130717-51-0 - Calbiochem

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
COX-1, COX-2

Product does not compete with ATP.

Reversible: no

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

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

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.

Legal Information

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