FR122047 (hydrate)

Cayman Chemical Item Number 10039

FR122047 (hydrate)

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.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

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).

Formal Name

1-[[4,5-bis(4-methoxyphenyl)-2-thiazolyl]carbonyl]-4-methyl-piperazine, monohydrochloride

Molecular Formula

C₂₃H₂₅N₃O₃S · HCl [H₂O]

Formula Weight

478.0

Formulation

A crystalline solid

Purity

≥98%

λ_max

234, 270, 344 nm

Stability

1 year

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

SMILES

Copy SMILES to clipboard

O=C(N1CCN(C)CC1)C2=NC(C3=CC=C(OC)C=C3)=C(S2)C4=CC=C(OC)C=C4.Cl

Background Reading

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).

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).

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).

Size

Price

Quantity

Subtotal

1 mg 
$14.00

$0.00

5 mg 
$63.00

$0.00

10 mg 
$112.00

$0.00

50 mg 
$490.00

$0.00

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$0.00

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FR122047 (hydrate)