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530617 TRPM Antagonist, M8-An - Calbiochem

A cell-permeable, highly potent antagonist of TRPM8 (IC₅₀ = 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells)

TRPM Antagonist, M8-An - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: TRPM8 Antagonist

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530617
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈H₁₆F₄N₂O₄

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      Description
      OverviewA cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC50 = 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC50 = 2.8 µM) and inhibit human TRPV1 (IC50 = 3.0 µM). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in naïve rats.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530617
      Brand Family Calbiochem®
      SynonymsTRPM8 Antagonist
      References
      ReferencesPatel, R., et al. 2014. J. Pharm. Exp. Ther. 345, in press.
      Product Information
      FormWhite solid
      Hill FormulaC₁₈H₁₆F₄N₂O₄
      Chemical formulaC₁₈H₁₆F₄N₂O₄
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetTRPM8
      Primary Target IC<sub>50</sub>10.9 nM
      Purity≥98% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      5.30617.0001 04055977260977

      Documentation

      TRPM Antagonist, M8-An - Calbiochem MSDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Patel, R., et al. 2014. J. Pharm. Exp. Ther. 345, in press.
      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.

      Revision27-June-2014 JSW
      SynonymsTRPM8 Antagonist
      DescriptionA cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC50 = 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC50 = 2.8 µM) and inhibit human TRPV1 (IC50 = 3.0 µM). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in naïve rats.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₈H₁₆F₄N₂O₄
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesPatel, R., et al. 2014. J. Pharm. Exp. Ther. 345, in press.