TRP Channel

Transient receptor potential (TRP) channel modulators act on cation channels that sense heat, cold and irritants. The mammalian family has six subfamilies, including vanilloid (TRPV), ankyrin (TRPA), canonical (TRPC) and melastatin (TRPM) channels. TRP channels respond to temperature, touch, osmotic changes and plant-derived compounds, so they are often described as cellular sensors. Cloning of the capsaicin receptor TRPV1 in 1997 identified it as a heat-activated ion channel in pain-sensing neurons. AMG517 and SB-705498 are TRPV1 antagonists, while A 967079 blocks TRPA1 and optovin activates TRPA1 when exposed to light. Pyr10 inhibits TRPC3, and Pico145 inhibits channels formed by TRPC1, TRPC4 and TRPC5. The spider toxin peptide GsMTx4, an inhibitor of mechanosensitive channels, is also listed under Piezo Channel.

9 Items

  • TRPML modulator 1
    Cat. No.
    A39682

    TRPML modulator 1

    TRPML modulator 1 is a selective modulator of the TRPML channel, known for its role in promoting autophagy. With an AC50 of less than 2 mM in the TFEB assay, it effectively enhances autophagic flux, making it a valuable tool for research applications focused on cellular degradation processes and lysosomal function. This compound is instrumental in studying the molecular mechanisms underlying autophagy-related diseases.

    1 mg
    $155.00
    5 mg
    $360.00
    All 6 sizes
  • ML-SI3
    Cat. No.
    A52217

    ML-SI3

    Synonyms: ML-SI3 (cis/trans mix)

    ML-SI3 is a modulator targeting TRPML1 and TRPML2 channels, exhibiting inhibitory activity with IC50 values of 4.7 μM and 1.7 μM, respectively. This compound effectively inhibits lysosomal calcium efflux and impairs TRPML1-mediated autophagy pathways. Additionally, the components of ML-SI3 serve as activators for TRPML2, with EC50 values of 3.3 μM and 9.4 μM, making it a valuable tool for studying TRPML channel dynamics and their roles in cellular processes.

    2 mg
    $35.00
    5 mg
    $55.00
    All 6 sizes
  • PQM-244
    Cat. No.
    A59352

    PQM-244

    PQM-244 is a multi-target modulator that primarily interacts with TRPV1 and cannabinoid receptors CB1 and CB2. It exhibits noteworthy peripheral antinociceptive properties, effectively addressing both neurogenic and inflammatory pain. Additionally, PQM-244 demonstrates antioxidant activity with an IC50 of 14.15 µM for radical scavenging of DPPH. This compound is suitable for research applications related to chronic pain and inflammatory conditions, including diabetes, atherosclerosis, and Alzheimer's disease.

    Out of stock

    All 3 sizes
  • TRPC6-PAM-C20
    Cat. No.
    A68738

    TRPC6-PAM-C20

    TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) targeting TRPC6 channels. This compound significantly enhances channel activation at low basal concentrations of diacylglycerol (DAG), facilitating increases in intracellular calcium ([Ca2+]i) levels in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 serves as an essential reagent for researchers investigating TRPC6-dependent signaling pathways and calcium dynamics.

    1 mg
    $140.00
    5 mg
    $375.00
    All 5 sizes
  • AMG-8562
    Cat. No.
    A68796

    AMG-8562

    AMG-8562 is a selective modulator of the TRPV1 ion channel, effectively inhibiting capsaicin activation while sparing heat-induced activation. This compound enhances TRPV1 activation at acidic pH levels and demonstrates significant analgesic properties by blocking capsaicin-induced flinching behaviors in various pain models. AMG-8562 has shown substantial efficacy in models of thermal hyperalgesia induced by complete Freund's adjuvant and skin incision, as well as in acetic acid-induced writhing assays, making it a valuable tool for pain research.

    25 mg
    $2,035.00
    50 mg
    $2,610.00
    All 3 sizes
  • TRPV4-KCa2.3 modulator 1
    Cat. No.
    A68800

    TRPV4-KCa2.3 modulator 1

    TRPV4-KCa2.3 modulator 1 is a modulator that enhances the TRPV4-KCa2.3 protein complex, exhibiting significant antihypertensive activity. This compound promotes hyperpolarization and vasodilation in endothelial cells. Its ability to influence vascular responses makes it a valuable tool for investigating hypertension and related cardiovascular disorders in research settings.

    Out of stock

    All 3 sizes
  • TRPC5 modulator-1
    Cat. No.
    A68818

    TRPC5 modulator-1

    TRPC5 modulator-1 is a potent modulator of the TRPC5 ion channel, demonstrating an IC50 of less than 1 nM. This compound is primarily utilized in research focused on neuropsychiatric disorders, providing insights into the mechanisms underlying these conditions. The modulation of TRPC5 may offer potential therapeutic strategies for addressing various neurological and psychiatric disorders.

    25 mg
    $1,800.00
    50 mg
    $2,285.00
    All 3 sizes
  • TRPV3 modulator-1
    Cat. No.
    A68879

    TRPV3 modulator-1

    TRPV3 modulator-1 is a selective modulator of the transient receptor potential vanilloid 3 (TRPV3) channel. It exhibits the ability to regulate TRPV3 activity, influencing calcium ion influx in response to thermal and chemical stimuli. This compound has potential applications in research related to pain sensation, skin physiology, and itch, making it a valuable tool for studying TRPV3-mediated signaling pathways.

    Out of stock

    All 3 sizes

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