PF-05105679 is a selective small-molecule modulator used in sensory biology and ion channel research, especially in studies focused on cold perception and TRPM8 signaling. In supplier catalogs and technical databases, it is commonly identified as PF-05105679 and CAS 1398583-31-7. This compound is particularly relevant in projects where researchers need a defined antagonist to evaluate TRPM8-dependent responses in mechanistic assays and translational pharmacology workflows. According to public chemical references, PF-05105679 molecular formula is C26H21FN2O3, and PF-05105679 chemical structure is associated with a quinoline-containing scaffold developed by Pfizer. These identifiers are useful for compound matching, analytical confirmation, and screening panel alignment across platforms.
Application of PF-05105679
In research settings, PF-05105679 is used in studies of cold sensation, pain signaling, ion channel pharmacology, and receptor-selective assay development. Its main application comes from its activity against TRPM8, a cold-sensitive ion channel involved in sensory transduction and linked to cold-related pain states. Because of this, the molecule is relevant for experiments that examine cold-triggered calcium signaling, sensory neuron activation, and pharmacological modulation of temperature-sensitive pathways. It is also useful for teams comparing selective TRPM8 antagonists during lead characterization and translational study design. Public sources additionally note that the compound entered clinical evaluation, which strengthens its value as a reference molecule in advanced discovery programs.
In Vitro
In vitro, PF-05105679 has been described as a selective TRPM8 blocker with reported IC50 values of 103 nM in general TRPM8 blocking assays, as well as 480 nM and 181 nM in cold- and WS-12-induced calcium flux assays in HEK293 cells expressing human TRPM8. Additional sources report more than 100-fold selectivity over a panel of receptors, ion channels, and enzymes, including TRPV1 and TRPA1. This profile makes the compound useful in mechanistic cellular studies where researchers need to distinguish TRPM8-driven responses from broader nonspecific channel effects.
In Vivo
In vivo, PF-05105679 has shown oral bioavailability and functional activity in animal models. Tocris reports that it reduces body temperature in rats and reverses cold-induced bladder capacity reduction in guinea pigs. Published pharmacology data also describe activity in guinea pig bladder ice water and menthol challenge models, supporting the view that this compound can connect in vitro TRPM8 inhibition with measurable physiological outcomes in living systems. That makes it relevant for translational studies focused on cold hypersensitivity and sensory pathway modulation.
Biochemical and Physiological Actions
Biochemically, PF-05105679 acts as an antagonist of TRPM8 ion channel activity and limits signaling associated with cold stimulation and TRPM8 agonist activation. Physiologically, this can influence cold sensation and temperature-related responses, which explains why the compound has been explored as a potential tool for cold-related pain research. Cross-species pharmacokinetic and pharmacodynamic work has also examined its effect on core body temperature, showing how TRPM8 blockade can translate into broader thermoregulatory outcomes.
Features and Benefits of PF-05105679
- Defined identifiers, including CAS 1398583-31-7, PF-05105679 molecular formula, and searchable PF-05105679 chemical structure
- Selective TRPM8 antagonism suitable for sensory biology, cold pain, and ion channel-focused studies
- Useful for researchers evaluating Pfizer PF-05105679 as a translational reference compound in validated workflows
For EBC-412105, PF-05105679 offers a practical balance of structural clarity, selective target activity, and in vivo relevance that supports confident use in modern TRPM8-focused research programs.
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