2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. TRP Channel
  5. TRPM Isoform
  6. TRPM Antagonist

TRPM Antagonist

TRPM Antagonists (7):

Cat. No. Product Name Effect Purity
  • HY-174825
    TRPM8 antagonist 4
    		Antagonist
    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.
  • HY-174846
    TRPM8 antagonist 4 prodrug
    		Antagonist
    TRPM8 antagonist 4 prodrug (Compound 8b) is an orally active CB2R agonist (EC50: 51.2 nM) and a weak TRPM8 antagonist. TRPM8 antagonist 4 prodrug is a prodrug of TRPM8 antagonist 4 (HY-174825). TRPM8 antagonist 4 prodrug exhibits anti-inflammatory and analgesic activities and can be used in the research of inflammation-related pain disorders.
  • HY-18662
    RQ-00203078
    		Antagonist 99.84%
    RQ-00203078 is a highly selective, potent and orally active TRPM8 antagonist with IC50s of 5.3 nM and 8.3 nM for rat and human TRPM8 channels, respectively. RQ-00203078 shows little inhibitory action against TRPV1, TRPA1, TRPV4, or TRPM2 channels.
  • HY-108451
    Ononetin
    		Antagonist 99.54%
    Ononetin, a natural deoxybenzoin, is a potent and selective TRPM3 channel blocker with an IC50 of 0.3 μM.
  • HY-144372
    TRPV1 antagonist 3
    		Antagonist 99.30%
    TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant.
  • HY-110181
    M8-B
    		Antagonist 99.89%
    M8-B is a potent transient receptor potential melastatin-8 (TRPM8) antagonist. M8-B blocks cold-induced and TRPM8-agonist-induced activation TRPM8 channels. M8-B decreases deep body temperature (Tb).
  • HY-172774
    TRPV1 antagonist 10
    		Antagonist
    TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.