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

C₂₃H₂₅N₃O₃S · xHCl

423.53 (free base basis)

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.

Cell permeable: yes
Target IC₅₀: 28 nM and 65 µM for human recombinant COX-1 and COX-2
Product does not compete with ATP.
Reversible: no
Primary Target
COX-1, COX-2

Toxicity: Standard Handling (A)

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

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.

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

100

≥98% (HPLC)

solid

Calbiochem^®

OK to freeze
desiccated (hygroscopic)
protect from light

pale yellow

1 M HCl: 2 mg/mL
water: 4 mg/mL
DMSO: 5 mg/mL

ambient

2-8℃

1S/C23H25N3O3S.ClH/c1-25-12-14-26(15-13-25)23(27)22-24-20(16-4-8-18(28-2)9-5-16)21(30-22)17-6-10-19(29-3)11-7-17;/h4-11H,12-15H2,1-3H3;1H

YWMAVHIKOAOSFM-UHFFFAOYSA-N

5 mg in Plastic ampoule
Packaged under inert gas

11 - Combustible Solids

WGK 3