1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
    Neuronal Signaling
  3. TRP Channel
  4. TRPV2 Isoform

TRPV2

TRPV2 (transient receptor potential vanilloid 2) is a non-selective cation channel of the TRPV family that mediates Ca2+ influx and participates in multiple cellular processes across neuronal and non-neuronal tissues[1][2]. Mechanistically, TRPV2 functions as a signaling hub linking extracellular physical or chemical stimuli to intracellular calcium-dependent responses, thereby regulating cell proliferation, survival, migration, differentiation, and immune activity[1][3]. TRPV2 is expressed in immune cells, where its translocation to the plasma membrane contributes to macrophage chemotaxis and phagocytosis, supporting innate immune responses through Ca2+-dependent signaling pathways[4]. In disease contexts, altered TRPV2 expression has been associated with multiple cancers, including urothelial carcinoma, prostate cancer, breast cancer, glioblastoma, and hematological malignancies, where the channel influences survival, proliferation, invasion, and therapeutic resistance pathways[3][5]. Compared with related isoforms, TRPV2 remains one of the least characterized members of the TRPV subfamily and exhibits distinct physiological properties that differentiate it from classical thermosensory TRPV channels, indicating specialized functions beyond canonical temperature sensing[1]. For experimental applications, TRPV2 can be activated by cannabinoids such as cannabidiol (CBD) and Δ9-tetrahydrocannabinol (Δ9-THC), which are widely used as pharmacological tools to investigate TRPV2-mediated Ca2+ signaling[6]. In contrast, tranilast has been reported as a TRPV2 inhibitor and is frequently employed to evaluate channel-specific functions in cellular and disease models[4].

TRPV2 Related Products (4):

Cat. No. Product Name Effect Purity
  • HY-B0545
    Probenecid
    Agonist 99.94%
    Probenecid is a potent and selective agonist of transient receptor potential vanilloid 2 (TRPV2) channels. Probenecid also inhibits pannexin 1 channels.
  • HY-132222
    SET2
    Antagonist 99.78%
    SET2 is a selective TRPV2 antagonist (IC50=0.46 μM). SET2 blocks the TRP channel and suppresses prostate cancer cells migration. SET2 reduces the lysophosphatidic acid (LPA, a TRPV2 activator)-induced cytoplasmic calcium increases.
  • HY-157131
    TRPV2-selective blocker 1
    Inhibitor 99.84%
    TRPV2-selective blocker 1 is a TRPV2-selective blocker that inhibits calcium influx and ionic currents. TRPV2-selective blocker 1 exhibits an IC50 of 6.3 μM against rat TRPV2, and shows no activity against TRPV1, TRPV3 or TRPV4 channels. TRPV2-selective blocker 1 attenuates macrophage phagocytosis, LPS-induced macrophage migration, and calcium microdomains generated by peripheral TRPV2. TRPV2-selective blocker 1 is non-cytotoxic and can be used to investigate the function of TRPV2 during immune processes.
  • HY-182896
    HKC54
    Antagonist
    HKC54 is a selective TRPV2 antagonist with an IC50 of 0.4 μM. HKC54 binds directly to TRPV2 and inhibits TRPV2-mediated calcium influx. HKC54 inhibits glioblastoma cell migration in vitro and breast cancer metastasis in vivo. HKC54 can be used for the research of breast cancer lung metastasis.