2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
    Neuronal Signaling
  4. TRP Channel
  5. TRPC4 Isoform

TRPC4

CCE1; TRP4

TRPC4 (transient receptor potential canonical 4) encodes a non-selective cation channel with moderate Ca2+ permeability and functions as a regulator of cellular calcium signaling and membrane excitability[1][2]. Mechanistically, TRPC4 can be activated downstream of Gαi-coupled receptors, Gαq-coupled receptors, and tyrosine kinase pathways, linking extracellular signals to calcium influx and downstream cellular responses[2]. TRPC4 participates in physiological processes including endothelial permeability, vasodilation, neurotransmitter release, and cell proliferation, highlighting its broad role in signal transduction networks[2]. In addition, TRPC4-containing channels contribute to calcium homeostasis and have been implicated in cellular migration and neuronal functions in experimental systems[3]. Disease-associated observations include elevated TRPC4 expression in focal cortical dysplasia type II and tuberous sclerosis complex cortical lesions, supporting continued investigation of TRPC4 in neurological disorders[3]. Compared with the closely related isoform TRPC5, TRPC4 is a distinct member of the TRPC subfamily, although both channels can participate in related signaling pathways and channel complexes[4][5]. TRPC4 also forms heteromeric assemblies, including TRPC1/TRPC4-containing channels, which contribute to neuronal and smooth-muscle functions in experimental models[5]. Structural studies further define TRPC4 as a tetrameric ion channel and provide a framework for mechanistic investigations and pharmacological modulation in future research applications[1].

TRPC4 Related Products (8):

Cat. No. Product Name Effect Purity
  • HY-133168
    Englerin A
    		Activator 99.50%
    Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca2+ influx and Ca2+ cell overload.
  • HY-12949
    ML204
    		Inhibitor 98.45%
    ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels.
  • HY-12949A
    ML204 hydrochloride
    		Inhibitor 99.74%
    ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca2+ channels.
  • HY-162090
    TRPC antagonist 1
    		Antagonist
    TRPC antagonist 1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50s of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TPRC6, and TRPC7, respectively. TRPC antagonist 1 displays noteworthy anti-glioblastoma efficacy in vitro against U87 cell lines.
  • HY-146155
    TRPC4/5-IN-1
    		Inhibitor
    TRPC4/5-IN-1 is a potent TRP channel 4/5 (TRPC4/5) inhibitor with IC50s of 2.06 μM and 0.54 μM, respectively. TRPC4/5-IN-1 can be used for proteinuric kidney diseases and skin inflammatory diseases research.
  • HY-184164
    JD03-02
    		Antagonist
    JD03-02 is an orally active, blood-brain barrier-permeable TRPC1/5 heterodimer inhibitor with an IC50 of 0.2 nM. JD03-02 preferentially binds to a unique ligand-binding pocket at the interface of TRPC1-TRPC5, exerts almost no inhibitory effect on TRPC5 homotetramers, and thus avoids side effects such as obesity and hyperkinesia. JD03-02 induces anxiolytic and antidepressant effects in mouse models. JD03-02 can be used in studies related to depression and anxiety disorders.
  • HY-173024
    TRPC4/5-IN-3
    		Inhibitor 99.65%
    TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87%.
  • HY-144429
    TRPC5-IN-4
    		Inhibitor
    TRPC5-IN-4 is potent and safe TRPC inhibitor with IC50 value of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively. TRPC5-IN-4 shows no damage on the cellular component of liver and kidney. TRPC5-IN-4 can be used for the research of chronic kidney disease (CKD).