FR 122047 HYDROCHLORIDE Chemical Properties

storage temp. 

2-8°C

solubility 

methylene chloride: 50 mg/mL, slightly hazy, yellow

form 

powder

color 

faint yellow

biological source

synthetic (organic)

Water Solubility 

Soluble to 10 mM in water

Safety Information

Safety Statements 

22-24/25

WGK Germany 

3

MSDS

• Language:English Provider:SigmaAldrich

FR 122047 HYDROCHLORIDE Usage And Synthesis

Description

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. 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. 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.

Uses

FR 122047 Hydrochloride is a selective cyclooxygenase-1 (Cox-1) inhibitor.

Biological Activity

Selective cyclooxygenase-1 (COX-1) inhibitor (IC 50 values are 0.028 and 65 μ M for COX-1 and COX-2 respectively). Antiplatelet, analgesic and anti-inflammatory following oral administration in vivo .

IC 50

COX-1: 28 nM (IC₅₀)

storage

Desiccate at +4°C

References

[1] TAKEHIRO OCHI  Toshio G  Yukio Motoyama. The analgesic effect profile of FR122047, a selective cyclooxygenase-1 inhibitor, in chemical nociceptive models[J]. European journal of pharmacology, 2000, 391 1: Pages 49-54. DOI: 10.1016/s0014-2999(00)00051-0
[2] MIWAKO DOHI . The anti-platelet actions of FR122047, a novel cyclooxygenase inhibitor[J]. European journal of pharmacology, 1993, 243 2: Pages 179-184. DOI: 10.1016/0014-2999(93)90378-u
[3] TAKEHIRO OCHI  Toshio G. Differential effect of FR122047, a selective cyclo-oxygenase-1 inhibitor, in rat chronic models of arthritis[J]. British Journal of Pharmacology, 2009, 135 3: 782-788. DOI: 10.1038/sj.bjp.0704511
[4] ANNA-KARIN JOHNSSON . COX-1 dependent biosynthesis of 15-hydroxyeicosatetraenoic acid in human mast cells[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2021, 1866 5: Article 158886. DOI: 10.1016/j.bbalip.2021.158886

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