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475889

MK-886

Name: MK-886
Brand: MM

≥99% (TLC), COX pathway blocker, solid

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

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この商品について

実験式（ヒル表記法）:

C₂₇H₃₃ClNO₂S · Na

CAS番号:

118414-82-7

分子量:

494.06

MDL number:

MFCD00876710

UNSPSC Code:

51111800

NACRES:

NA.77

Assay:

≥99% (TLC)

Form:

solid

Storage condition:

OK to freeze

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特性

製品名

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.

Quality Segment

100

assay

≥99% (TLC)

form

solid

potency

102 nM IC₅₀

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze

color

white

solubility

DMSO: 25 mg/mL, ethanol: 25 mg/mL

shipped in

ambient

storage temp.

10-30°C

SMILES string

S(CCCC)c1c2c([n](c1CC(C)(C)C(=O)O)Cc3ccc(cc3)Cl)ccc(c2)C(C)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

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
leukotreine biosybthesis

Product does not compete with ATP.

Reversible: no

Other Notes

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.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

保管分類

11 - Combustible Solids

一体何が起きているの？

WGK 1

引火点 (F)

Not applicable

引火点（°C）