236005

COX-1 Inhibitor, FR122047

The COX-1 Inhibitor, FR122047, also referenced under CAS 130717-51-0, controls the biological activity of COX-1. This small molecule/inhibitor is primarily used for Cell Signaling applications.

• Sinonimo/i: COX-1 Inhibitor, FR122047, FR 122047, 1-[(4,5-Bis(4-methoxyphenyl-2-thiazoyl)carbonyl]-4-methylpiperazine, Hydrochloride, 4,5-Bis(4-methoxyphenyl-2-[(1-methylpiperazin-4-yl)carbonyl]thiazole, Hydrochloride
• Formula empirica (notazione di Hill): C₂₃H₂₅N₃O₃S · xHCl
• Numero CAS: 130717-51-0
• Peso molecolare: 423.53 (free base basis)
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥98% (HPLC)
• Forma fisica: solid
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze; desiccated (hygroscopic); protect from light
• Colore: pale yellow
• Solubilità: 1 M HCl: 2 mg/mL; water: 4 mg/mL; DMSO: 5 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 2-8°C
• InChI: 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

Descrizione

Descrizione generale

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.

Azioni biochim/fisiol

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

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

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

Altre note

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.

Note legali

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

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable