TRPC3

TRP3

TRPC3 (Transient Receptor Potential Canonical 3) is a member of the canonical TRP channel family that mediates Ca²⁺ and other cation influx downstream of phospholipase C (PLC)-coupled receptor activation, thereby regulating intracellular calcium signaling and diverse cellular responses^[1]. TRPC3 functions as a diacylglycerol-sensitive cation channel and is closely linked to PLC-dependent signaling pathways that control neuronal activity, cellular growth, and stress-responsive signaling networks^[2]^[3]. Mechanistically, TRPC3-mediated Ca²⁺ entry promotes activation of the calcineurin/NFAT pathway, a key signaling axis involved in transcriptional regulation and cellular remodeling^[4]^[5]. In disease-related models, increased TRPC3 expression or gain-of-function activity has been associated with cardiac hypertrophy, heart failure, myocardial fibrosis, and pathological remodeling, highlighting its importance in calcium-dependent disease mechanisms^[4]^[5]. In the nervous system, TRPC3 acts downstream of metabotropic glutamate receptor 1 (mGluR1), contributes to Purkinje neuron function, and regulates signaling processes essential for neuronal viability and motor coordination^[6]^[7]. Compared with closely related TRPC6 and TRPC7 isoforms, TRPC3 possesses distinct pharmacological properties that enable selective experimental targeting^[1]^[8]. For research applications, the pyrazole-derived compound Pyr3 directly and selectively inhibits TRPC3 channels, suppresses TRPC3-dependent calcium influx and downstream signaling, and has become a widely used tool for dissecting TRPC3-specific biological functions in cellular and animal models^[1]^[8]^[9].

References:

[1]. Kiyonaka S, et al. Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proc Natl Acad Sci U S A. 2009 Mar 31;106(13):5400-5. [Content Brief]

[2]. Aslam N, et al. TRPC3 Channel Activity and Viability of Purkinje Neurons can be Regulated by a Local Signalosome. Front Mol Biosci. 2022 Feb 21;9:818682. [Content Brief]

[3]. Tiapko O, et al. TRPC3 as a Target of Novel Therapeutic Interventions. Cells. 2018 Jul 22;7(7):83. [Content Brief]

[4]. Lee MJ, et al. Time to HIV rebound after infusion of long-acting broadly neutralising antibodies 3BNC117-LS and 10-1074-LS and analytical treatment interruption (the RIO trial): a double-blind, randomised, placebo-controlled trial. Lancet HIV. 2026 May 27:S2352-3018(26)00059-7. [Content Brief]

[5]. Zhang S, et al. Discovery of a Highly Selective and Potent TRPC3 Inhibitor with High Metabolic Stability and Low Toxicity. ACS Med Chem Lett. 2021 Mar 5;12(4):572-578. [Content Brief]

[6]. Munakata M, et al. Transient receptor potential canonical 3 inhibitor Pyr3 improves outcomes and attenuates astrogliosis after intracerebral hemorrhage in mice. Stroke. 2013 Jul;44(7):1981-7. [Content Brief]

TRPC3 Related Products (10):

By Type:	Pan (3) Selective (5)
By Effects:	Inhibitors (6) Agonists (2) Antagonist (1) Activator (1)

Cat. No.	Product Name	Effect	Purity

HY-111098

GSK1702934A	Agonist	99.52%
GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.

HY-19408

Pyr10	Inhibitor	99.95%
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca²⁺ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC₅₀ of 0.72 μM (IC₅₀ of 13.08 μM for store operated Ca²⁺ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels.

HY-101795

Larixyl acetate	Inhibitor	99.44%
Larixyl acetate is a potent and selective TRPC6 inhibitor with IC₅₀ values of 0.58 μM and 6.83 μM against hTRPC6-YFP and hTRPC3-YFP, respectively. Larixyl acetate prevents HPV and is effective in protecting against traumatic brain injury-induced systemic endothelial dysfunction.

HY-133012

GFB-8438	Inhibitor	99.74%
GFB-8438 is a potent and subtype selective TRPC5 inhibitor, with IC₅₀s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively. GFB-8438 shows excellent selectivity against TRPC6, other TRP family members, NaV 1.5, as well as limited activity against the hERG channel. GFB-8438 protects mouse podocytes from injury induced by protamine sulfate model.

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.

HY-138668

JW-65	Inhibitor	99.05%
JW-65 is a selective TRPC3 channel inhibitor with favorable blood-brain barrier penetration. JW-65 directly binds to human TRPC3 protein and modulates calcium signaling to reduce seizure susceptibility. JW-65 reduces seizure incidence, severity, and duration while prolonging seizure latency in multiple seizure models. JW-65 alleviates Aβ‑induced neuronal damage. JW-65 serves as a valuable tool for research on epilepsy, seizure disorders, and Alzheimer’s disease.

HY-161766

L687	Activator	99.49%
L687 is a potent activator of TRPC3/C6/C7 that can induce cellular uptake of oligonucleotides.

HY-147357

TRPC3/6-IN-1	Inhibitor
TRPC3/6-IN-1 is a potent selectivity blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC₅₀ values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure.

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-179489

TRPC3 agonist-1	Agonist
TRPC3 agonist-1 (compound 4n) is a selective and competitive TRPC3 channel agonist. TRPC3 agonist-1 binds at L2 site of hTRPC3.

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