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

Overview

Replacement Information

Key Specifications Table

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

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475889-5MG
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      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

      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.