TRPM8 antagonist 4

TRPM8 antagonist 4 is a CB2R partial agonist (EC50=54.2 nM, Ki=3.2 μM) and TRPM8 antagonists (IC50=42.3 nM) with high functional selectivity and good physicochemical properties. TRPM8 antagonist 4 has significant anti-inflammatory and analgesic effects and good safety, reduces the mRNA expression of TNF-α, IL-6, and IL-1β[1].

Product Specifications

UNSPSC

12352005

Target

Cannabinoid Receptor; Interleukin Related; TNF Receptor; TRP Channel

Related Pathways

Apoptosis; GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Smiles

O=C(N)C1=C(O)C=C(OC/C=C(C)/CC/C=C(C)/C)C=C1C2CC2

Molecular Formula

C20H27NO3

Molecular Weight

329.43

References & Citations

[1]Yang W, et al. Identification of Cannabigerol-Derived Dual CB2 Receptor Agonists and TRPM8 Antagonists with Anti-Inflammatory and Analgesic Activities. J Med Chem. 2025 Jul 10;68 (13) :13335-13357.