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475889 MK-886 - CAS 118414-82-7 - Calbiochem

475889
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
118414-82-7C₂₇H₃₃ClNO₂S · Na

Products

Catalogue NumberPackaging Qty/Pack
475889-5MG Plastic ampoule 5 mg
Description
OverviewA 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 µM, 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 µM MK-886). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, MK-886 does not cause gastrointestinal damages when applied in vivo.
Catalogue Number475889
Brand Family Calbiochem®
Synonyms3-[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
References
ReferencesKoeberle, 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.
Product Information
CAS number118414-82-7
ATP CompetitiveN
FormWhite solid
Hill FormulaC₂₇H₃₃ClNO₂S · Na
Chemical formulaC₂₇H₃₃ClNO₂S · Na
ReversibleN
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary Targetleukotreine biosybthesis
Primary Target IC<sub>50</sub>102 nM
Purity≥99% by TLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +15°C to +30°C
Do not freeze Ok to freeze
Special InstructionsUnstable in solution; reconstitute just prior to use.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
475889-5MG 04055977203592

Documentation

MK-886 - CAS 118414-82-7 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

MK-886 - CAS 118414-82-7 - Calbiochem Certificates of Analysis

TitleLot Number
475889

References

Reference overview
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.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision21-January-2013 JSW
Synonyms3-[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
DescriptionA 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 µM, 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 µM MK-886). Unlike NSAIDs (nonsteroidal antiinflammatory drugs) that target only COX pathway, MK-886 does not cause gastrointestinal damages when applied in vivo.
FormWhite solid
CAS number118414-82-7
Chemical formulaC₂₇H₃₃ClNO₂S · Na
Structure formulaStructure formula
Purity≥99% by TLC
SolubilityDMSO (25 mg/ml) or Ethanol (25 mg/ml)
Storage +15°C to +30°C
Do Not Freeze Ok to freeze
Special InstructionsUnstable in solution; reconstitute just prior to use.
Toxicity Standard Handling
ReferencesKoeberle, 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.