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

475889
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₇H₃₃ClNO₂S · Na 118414-82-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      475889-5MG
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          Plastic ampoule 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.