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

TRP Channel

Transient receptor potential channels

TRP Channel

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TRP Channel (Transient receptor potential channel) is a group of ion channels located mostly on the plasma membrane of numerous human and animal cell types. There are about 28 TRP channels that share some structural similarity to each other. These are grouped into two broad groups: Group 1 includes TRPC ("C" for canonical), TRPV ("V" for vanilloid), TRPM ("M" for melastatin), TRPN, and TRPA. In group 2, there are TRPP ("P" for polycystic) and TRPML ("ML" for mucolipin). Many of these channels mediate a variety of sensations like the sensations of pain, hotness, warmth or coldness, different kinds of tastes, pressure, and vision. TRP channels are relatively non-selectively permeable to cations, including sodium, calcium and magnesium. TRP channels are initially discovered in trp-mutant strain of the fruit fly Drosophila. Later, TRP channels are found in vertebrates where they are ubiquitously expressed in many cell types and tissues. TRP channels are important for human health as mutations in at least four TRP channels underlie disease.

TRP Channel Isoform Specific Products:

TRP Channel Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-N0637A
    (±)-Eriodictyol
    		Inhibitor 99.9%
    (±)-Eriodictyol ((±)-Huazhongilexone; Dihydroluteolin) is an orally active TRPV1 receptor antagonist (IC50=44-47 nM, rTRPV1) with antioxidant and anti-inflammatory activities. (±)-Eriodictyol effectively inhibits lipid peroxidation and the release of proinflammatory cytokines by specifically antagonizing the TRPV1 receptor and activating the Nrf2 signaling pathway. (±)-Eriodictyol reduces the levels of ICAM-1, VEGF, eNOS and TNF-α in the retina and maintains the integrity of the blood-retinal barrier. (±)-Eriodictyol alleviates oxidative stress-induced apoptosis and hyperalgesia, enhances the activity and cytotoxicity of immune cells (such as B lymphocytes, NK cells and macrophages), and increases the levels of antioxidant enzymes simultaneously. (±)-Eriodictyol can be used in the research of diabetic retinopathy, acute lung injury and various pain-related diseases.
    (±)-Eriodictyol
  • HY-148236
    BAY-390
    		Inhibitor 99.74%
    BAY-390, a chemical probe, is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC50s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammation.
    BAY-390
  • HY-P1651A
    SOR-C13 TFA
    		Antagonist 99.32%
    SOR-C13 TFA, a carboxy-terminal truncated peptide, is a high-affinity TRPV6 antagonist with an IC50 value of 14 nM. TRPV6 is a non-voltage gated calcium channel that is associated with malignancy and poor prognosis in breast cancer. SOR-C13 TFA has anticancer activity.
    SOR-C13 TFA
  • HY-108460
    A-784168
    		Inhibitor 99.79%
    A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration.
    A-784168
  • HY-16162A
    D-3263 hydrochloride
    		Agonist 98.12%
    D-3263 hydrochloride is an enteric-coated, orally bioavailable (transient receptor potential melastatin member 8) TRPM8 agonist.
    D-3263 hydrochloride
  • HY-109087
    Elismetrep
    		Antagonist 99.42%
    Elismetrep (MT-8554) is a TRPM8 antagonist. Elismetrep reduces the frequency of vasomotor symptoms. Elismetrep can be used for study of pain.
    Elismetrep
  • HY-B0985
    Phenazopyridine hydrochloride
    		Antagonist 99.55%
    Phenazopyridine hydrochlorideis a competitive SARM1 inhibitor, with IC50 145 μM. Phenazopyridine hydrochlorideis a TRPM8 antagonist. Phenazopyridine hydrochloride has a local anesthetic/analgesic effect. Phenazopyridine hydrochlorideis used to relieve painful symptoms of conditions such as cystitis and urethritis. Phenazopyridine hydrochloridecan promote neuronal differentiation and can also be used in the study of traumatic brain injury, peripheral neuropathy and neurodegenerative diseases.
    Phenazopyridine hydrochloride
  • HY-139192
    Brophenexin
    		Inhibitor 98.74%
    Brophenexin (compound 8) is a potent NMDAR/TRPM4 interaction interface inhibitor. Brophenexin shows neuroprotective activity. Brophenexin prevents NMDA-induced cell death and mitochondrial dysfunction in hippocampal neurons, with an IC50 of 2.1 μM. Brophenexin protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell loss.
    Brophenexin
  • HY-116291
    4α-Phorbol 12,13-didecanoate
    		Agonist 99.30%
    4α-Phorbol 12,13-didecanoate (4αPDD) is a transient receptor potential vanilloid 4 (TRPV4) agonist. 4α-Phorbol 12,13-didecanoate can promote Ca2+ influx, induce ATP release and function as an osmoreceptor. 4α-Phorbol 12,13-didecanoate can inhibit water intake and increase maximal micturition pressure in rats. 4α-Phorbol 12,13-didecanoate can be used for the researches of inflammation and infection, such as chikungunya virus (CHIKV).
    4α-Phorbol 12,13-didecanoate
  • HY-108329
    AM-0902
    		Antagonist 99.73%
    AM-0902 is a potent, selective transient receptor potential A1 (TRPA1) antagonist with IC50s of 71 and 131 nM for rTRPA1 and hTRPA1, respectively.
    AM-0902
  • HY-109061B
    Lazertinib mesylate
    		Activator 99.85%
    Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia.
    Lazertinib mesylate
  • HY-108464A
    Phenamil methanesulfonate
    		Inhibitor 98.1%
    Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
    Phenamil methanesulfonate
  • HY-104059
    AMG2850
    		Antagonist 99.89%
    AMG2850 is a potent, orally bioavailable and selective transient receptor potential melastatin 8 (TRPM8) antagonist.
    AMG2850
  • HY-134819
    (1S,2S)-ML-SI3
    		Inhibitor 99.96%
    (1S,2S)-ML-SI3 is a trans-isomer of ML-SI3 that targets all three isoforms of TRPML. (1S,2S)-ML-SI3 is an activator of TRPML2 and TRPML3 (EC50=2.7 μM/10.8 μM) and a potent inhibitor of TRPML1 (IC50=5.9 μM).
    (1S,2S)-ML-SI3
  • HY-110181
    M8-B
    		Antagonist 99.74%
    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).
    M8-B
  • HY-B1239
    Drofenine hydrochloride
    		98.10%
    Drofenine (Cycloadiphene; Hexahydroadiphenine) hydrochloride is an brain-penetrant antispasmodic agent. Drofenine hydrochloride is a Kv2.1 channel inhibitor with human IC50 of 9.53 μM. Drofenine hydrochloride is a butyrylcholinesterase (BChE) inhibitor with Ki of 0.003 mM, and is a TRPV3 activator. Drofenine hydrochloride blocks Kv2.1-dependent potassium efflux, inhibits Kv2.1/JNK/NF-κB and IkBa/NF-kB signaling, suppresses Kv2.1 mRNA/protein expression. Drofenine suppresses oligomeric Aβ-induced microglial NLRP3 inflammasome activation and neuronal Tau hyperphosphorylation, improves cognitive impairment, promotes neurite outgrowth. Drofenine hydrochloride induces calcium influx in keratinocytes and exert cytotoxicity against keratinocytes. Drofenine hydrochloride ameliorates diabetic peripheral neuropathy -like pathology. Drofenine hydrochloride can be used for the researches of Alzheimer's disease, diabetic peripheral neuropathy and smooth muscle spasm.
    Drofenine hydrochloride
  • HY-136363
    MDR-652
    		Agonist 98.08%
    MDR-652 is a highly specific and efficacious transient receptor potential vanilloid 1 (TRPV1) ligand with agonist activity. The Kis are 11.4 and 23.8 nM for hTRPV1 and rTRPV1, respectively. The EC50s are 5.05 and 93 nM for hTRPV1 and rTRPV1, respectively. Potent topical analgesic activity.
    MDR-652
  • HY-N6962
    α-Spinasterol
    		Antagonist 99.90%
    α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC50 values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice.
    α-Spinasterol
  • HY-N2318
    Podocarpic acid
    		Agonist 99.78%
    Podocarpic acid is a natural product, which has the best all-round positive effect and acts as a novel TRPA1 activator.
    Podocarpic acid
  • HY-75161R
    (-)-Menthol (Standard)
    		Activator
    (-)-Menthol (Standard) is the analytical standard of (-)-Menthol. This product is intended for research and analytical applications. (-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca2+-permeable nonselective cation channel, to increase [Ca2+]i. Antitumor activity.
    (-)-Menthol (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
TRP Channel Isoform Comparison

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