1398583-31-7

PF-05105679 is an orally active and selective TRPM8 antagonist with an IC50 of 103 nM. PF-05105679 has the potential for cold-related pain[1].

PF-05105679 is an antagonist of the TRP (transient receptor potential) channelalso known as the cold and menthol receptor 1 (CMR1)with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling painand pain-alleviating effects matched those of oxycodone for about one hour after administration.''PF-05105679 is an antagonist of the TRP (transient receptor potential) channelalso known as the cold and menthol receptor 1 (CMR1)with an IC50 value of 103 nM. PF-05105679 is in clinical trials for neuropathic pain. Participants taking PF-05105679 could hold their hands in a bucket of ice water for a long time before feeling painand pain-alleviating effects matched those of oxycodone for about one hour after administration.
Transient receptor potential cation channel subfamily M member 8 (TRPM8) antagonistPF-05105679 [(

TRPM8: 103 nM (IC₅₀)

[1] Andrews MD, et al. Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain. ACS Med Chem Lett. 2015 Jan 30;6(4):419-24. DOI:10.1021/ml500479v