FR122047 (hydrochloride)

FR122047 is a selective inhibitor of COX-1. The IC₅₀ values for inhibition of human COX-1 and COX-2 are 0.028 and 65 µM, respectively.¹ In human platelet-rich plasma, FR122047 inhibits arachidonic acid, collagen, and ADP-induced platelet aggregation with an IC₅₀ of 180-200 nM, which is nearly 100 times more potent than aspirin.² Unlike aspirin, FR122047 does not induce gastric damage upon oral administration at doses (100 mg/kg) far in excess of the dose needed for complete suppression of platelet COX-1. In some models of inflammation, such as collagen-induced arthritis in the rat, FR122047 has an anti-inflammatory effect, implying a role for COX-1 in these models.³

WARNING This product is not for human or veterinary use.

1. Ochi, T., Motoyama, Y., and Goto, T. The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models. Eur. J. Pharmacol. 391, 49-54 (2000).

2. Dohi, M., Sakata, Y., Seki, J., et al. The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor. Eur. J. Pharmacol. 243, 179-184 (1993).

3. Ochi, T., and Goto, T. Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis. Br. J. Pharmacol. 135, 782-788 (2002).

Johnsson, A.-K., Rönnberg, E., Fuchs, D., et al. COX-1 dependent biosynthesis of 15-hydroxyeicosatetraenoic acid in human mast cells. Biochim. Biophys. Acta Mol. Cell Biol. Lipids 1866(5), 158886 (2021).

Johnsson, A.K., Choi, J.H., Rönnberg, E., et al. Selective inhibition of prostaglandin D₂ biosynthesis in human mast cells to overcome need for multiple receptor antagonists: Biochemical consequences. Clin. Exp. Allergy 51(4), 594-603 (2021).