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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

530617
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₈H₁₆F₄N₂O₄

Products

Catalogue NumberPackaging Qty/Pack
5.30617.0001 Glass bottle 10 mg
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 SDS

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.