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.

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₂₃H₂₅N₃O₃S · xHCl
• Numer CAS: 130717-51-0
• Masa cząsteczkowa: 423.53 (free base basis)
• Kod UNSPSC: 51111800
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Formularz: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; desiccated (hygroscopic); protect from light
• kolor: pale yellow
• rozpuszczalność: 1 M HCl: 2 mg/mL; water: 4 mg/mL; DMSO: 5 mg/mL
• Warunki transportu: ambient
• temp. przechowywania: 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
• Klucz InChI: YWMAVHIKOAOSFM-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

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

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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.

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable