TRPC5

CCE2; TRP5

TRPC5 is a receptor-activated Ca²⁺-permeable cation channel within the TRPC family, linking extracellular receptor stimulation to intracellular ion entry^[1]. Mechanistically, GPCR signaling can act through Gα_i3, which binds the TRPC5 ankyrin-repeat edge and increases PIP₂ sensitivity, thereby facilitating channel opening^[2]. In disease-relevant models, TRPC5 supports amygdala-dependent innate fear behavior, and kidney studies identify TRPC5-mediated Rac1 activation, synaptopodin destabilization, podocyte cytoskeletal remodeling, and albuminuria^[3]^[4]. Compared with related isoforms, TRPC5 forms homotetramers, whereas the human TRPC1/C5 heteromer contains one TRPC1 and three TRPC5 subunits, producing an asymmetric selectivity filter and lower gate distinct from the TRPC5 homomer^[5]. For experimental applications, AC1903 specifically blocked TRPC5 channel activity in proteinuric rat glomeruli and suppressed severe proteinuria and podocyte loss in FSGS models^[6]. Structural inhibitor studies further mapped human TRPC5 complexes with clemizole and HC-070, supporting rational use of TRPC5 inhibitors in channel-function and disease-model research^[7].

References:

[1]. Hofmann T, et al. Subunit composition of mammalian transient receptor potential channels in living cells. Proc Natl Acad Sci U S A. 2002 May 28;99(11):7461-6. [Content Brief]

[2]. Won J, et al. Molecular architecture of the Gα_i-bound TRPC5 ion channel. Nat Commun. 2023 May 3;14(1):2550. [Content Brief]

[3]. Riccio A, et al. Essential role for TRPC5 in amygdala function and fear-related behavior. Cell. 2009 May 15;137(4):761-72. [Content Brief]

[4]. Schaldecker T, et al. Inhibition of the TRPC5 ion channel protects the kidney filter. J Clin Invest. 2013 Dec;123(12):5298-309. [Content Brief]

[5]. Kim SH, et al. Molecular architecture of the human TRPC1/C5 heteromeric channel. Nat Commun. 2025 Dec 10;17(1):317. [Content Brief]

[6]. Zhou Y, et al. A small-molecule inhibitor of TRPC5 ion channels suppresses progressive kidney disease in animal models. Science. 2017 Dec 8;358(6368):1332-1336. [Content Brief]

[7]. Song K, et al. Structural basis for human TRPC5 channel inhibition by two distinct inhibitors. Elife. 2021 Mar 8;10:e63429. [Content Brief]

TRPC5 Related Products (14):

By Type:	Pan (4) Selective (5)
By Effects:	Inhibitors (8) Antagonists (2) Activator (1) Modulators (3)

Cat. No.	Product Name	Effect	Purity

HY-17386

Rosiglitazone	Modulator	99.94%
Rosiglitazone (BRL 49653) is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM), with blood-brain barrier permeability. Rosiglitazone is an TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone can be used in the research of obesity and diabetes, senescence, ovarian cancer.

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-17386A

Rosiglitazone hydrochloride	Modulator	99.81%
Rosiglitazone (BRL 49653) hydrochloride is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone hydrochloride is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone hydrochloride can be used in the research of obesity and diabetes, senescence, ovarian cancer.

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-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-17386B

Rosiglitazone potassium	Modulator	99.13%
Rosiglitazone (BRL 49653) potassium is an orally active selective PPARγ agonist (EC₅₀: 60 nM, K_d: 40 nM). Rosiglitazone potassium is a TRPC5 activator (EC₅₀: 30 μM) and TRPM3 inhibitor. Rosiglitazone potassium can be used in the research of obesity and diabetes, senescence, ovarian cancer.

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-172106

TRPC5-IN-5	Inhibitor
TRPC5-IN-5 (Compound ph8) is a TRPC5 inhibitor (IC₅₀: 1.28 μM). TRPC5-IN-5 can be used for research of neurological diseases and renal diseases.

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-162584

TRPC5-IN-6	Inhibitor
TRPC5-IN-6 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC₅₀ value of 81 nM. TRPC5-IN-6 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD).

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).

HY-18101

BD-1063	Inhibitor
BD-1063 is a selective σ-1 receptor antagonist with inhibitory activity against TRPC5 and TRPM3. BD-1063 exerts anti-hyperalgesic and anti-allodynic effects by inhibiting sustained calcium influx mediated by TRPC5 and TRPM3, and reverses the effects of Carrageenan (HY-125474). BD-1063 also significantly reduces excessive ethanol self-administration behavior. BD-1063 is widely used in studies on the mechanisms underlying neuropathic pain, inflammatory hyperalgesia, and alcohol abuse and dependence.

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