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.

• 別名: 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
• 実験式（ヒル表記法）: C₂₇H₃₃ClNO₂S · Na
• CAS番号: 118414-82-7
• 分子量: 494.06
• UNSPSCコード: 51111800
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥99% (TLC)
• 形状: solid
• 有効性: 102 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze
• 色: white
• 溶解性: DMSO: 25 mg/mL; ethanol: 25 mg/mL
• 輸送温度: ambient
• 保管温度: 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)
• InChI Key: VFMGWQLOCZBFCK-UHFFFAOYSA-N

詳細

詳細

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.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
leukotreine biosybthesis

Product does not compete with ATP.

Reversible: no

警告

Toxicity: Standard Handling (A)

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable