TRPM8 antagonist 4 

TRPM8 antagonist 4 is a CB2R partial agonist (EC₅₀=54.2 nM, K_i=3.2 μM) and TRPM8 antagonists (IC_{50=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].}

TRPM8 antagonist 4 (compound 6b) exhibits neither antagonistic nor agonistic activity at the CB1R in the HTRF cAMP assay^[1].

TRPM8 antagonist 4 (1 nM-1000 nM) inhibits hTRPM8 currents induced by 30.0 μM menthol in HEK293 cells, with IC₅₀=42.3 nM^[1].

TRPM8 antagonist 4 (1 μM-1 M) binds to CB2R by radioligand competition assay^[1].

TRPM8 antagonist 4 (0.3 μM, 8h) reduces the mRNA expression of TNF-α, IL-6, and IL-1β in LPS-stimulated RAW264.7 macrophages^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

TRPM8 antagonist 4 (compound 6b) (2.5 mg/kg, i.p., once) shows anti-inflammatory effects in LPS (HY-D1056)-induced inflammation in C57BL/6J mice model^[1].

TRPM8 antagonist 4 (5 mg/kg, i.p., once) exhibits pronounced analgesic effects in the Acetic acid (HY-Y0319)-induced in C57BL/6J mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

329.43

C₂₀H₂₇NO₃

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]