475889

MK-886

A cell-permeable, orally active NSAID that blocks cellular Cox pathway PGE2 production by inhibiting COX-1 and mPGES-1, but not COX-2, activity, as well as suppresses cellular 5-LO pathway activation by inhibiting FLAP, rather than 5-LO, activity.

• Sinonimo/i: MK-886, 3-[1-( p-Chlorobenzyl)-5-(isopropyl)-3- t-butylthioindol-2-yl]-2,2-dimethylpropanoic Acid, Na, COX-1 Inhibitor III, FLAP Inhibitor I, MK886, mPGES-1 Inhibitor I
• Formula empirica (notazione di Hill): C₂₇H₃₃ClNO₂S · Na
• Numero CAS: 118414-82-7
• Peso molecolare: 494.06
• Codice UNSPSC: 51111800
• NACRES: NA.77

Proprietà

• Livello qualitativo: 100
• Saggio: ≥99% (TLC)
• Forma fisica: solid
• Potenza: 102 nM IC₅₀
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: white
• Solubilità: DMSO: 25 mg/mL; ethanol: 25 mg/mL
• Condizioni di spedizione: ambient
• Temperatura di conservazione: 10-30°C
• InChI: 1S/C27H34ClNO2S/c1-6-7-14-32-25-22-15-20(18(2)3)10-13-23(22)29(17-19-8-11-21(28)12-9-19)24(25)16-27(4,5)26(30)31/h8-13,15,18H,6-7,14,16-17H2,1-5H3,(H,30,31); VFMGWQLOCZBFCK-UHFFFAOYSA-N

Descrizione

Descrizione generale

A cell-permeable, orally active NSAID (nonsteroidal antiinflammatory drug) that blocks cellular Cox pathway PGE2 (prostaglandin E₂) production by inhibiting COX-1 and mPGES-1 (microsomal PGE₂ synthase-1), but not COX-2, activity (IC₅₀ = 8, 2, and 58 M, respectively), as well as suppresses cellular 5-LO (5-Lypoxygenase; Cat. No. 437996) pathway activation by inhibiting FLAP (5-LO-activating protein), rather than 5-LO, activity (<10% by 1 M MK-886). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, MK-886 does not cause gastrointestinal damages when applied in vivo.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
leukotreine biosybthesis

Product does not compete with ATP.

Reversible: no

Attenzione

Toxicity: Standard Handling (A)

Altre note

Koeberle, A., et al. 2009. Eur. J. Pharmacol.608, 84.
Koeberle, A., et al. 2008. J. Pharmacol. Exp. Ther.326, 975.
Fisher, L., et al. 2007. Br. J. Pharmacol.152, 471.
Ford-Hutchinson, A.W., et al. 1993. Can. J. Physiol. Pharmacol. 71, 806.
Ford-Hutchinson, A.W. 1991. Trends Pharmacol.12, 68.
Dixon, R.A., et al. 1990. Nature 343, 282.
Rouzer, C.A., et al. 1990. J. Biol. Chem.265, 1436.

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 1
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable