trpc3

TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

GSK1702934A, a selective TRPC3 agonist, modulates cardiac contractility and arrhythmogenesis through TRPC3 activation.

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

Pyr3 is a selective transient receptor potential canonical channel 3 inhibitor. Pyr3 inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner(IC50 = 700 nM).

TRPC3 agonist-1 (compound 4n) is a selective competitive activator of the TRPC3 channel, binding specifically to the L2 site of hTRPC3.

TRPC3/6-IN-1 is a highly potent and selective inhibitor that blocks the activity of canonical transient receptor channels TRPC3 and TRPC6, showing significant potency against human isoforms hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. This compound is valuable for research on chronic models of heart failure [1].

TRPC3/6-IN-2 is a potent inhibitor of TRPC3 and TRPC6, with IC50 values of 16 nM and 29.8 nM, respectively [1].

IGS-1.76 exhibits pronounced affinity towards hNCS-1 and effectively modulates the interaction between hNCS-1 and Ric8a. Moreover, IGS-1.76 proficiently inhibits the complex formed by human NCS-1 and Ric8a.

Larixyl acetate is a bioactive chemical.

TRPC antagonist1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50 values of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7, respectively. It demonstrates significant anti-glioblastoma efficacy in vitro against the U87 cell line.

GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels.

GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.

BI-749327 is a high selectivity and orally bioavailable antagonist of TRPC6 (IC50s: 13 nM, 19 nM and 15 nM for mouse, human and guinea pig TRPC6).

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide) is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.

JW-65 (compound 20) is an inhibitor of TRPC3. It is utilized in research related to neurological and cardiovascular diseases.

TRPC6 antagonist-1 (X26) is a TRPC6 inhibitor with IC50 values of 0.97 μM for TRPC6, 3.93 μM for TRPC3, 5.77 μM for TRPC5, and 4.37 μM for TRPC7. Additionally, TRPC6 antagonist-1 hinders TGF-β1-induced myofibroblast differentiation, thereby mitigating renal fibrosis.

PPZ1 is a novel DAG-activated TRPC3/TRPC6/TRPC7 channels activator.

PPZ2 is a novel DAG-activated TRPC3/TRPC6/TRPC7 channels activator.

OptoDArG is an optogenetic tool compound used to reversibly regulate DAG (diacylglycerol)-related signaling pathways under specific light conditions. It acts as a potent agonist of lipid-gated ion channels (TRPC3/6/7), mimicking the activating function of endogenous DAG, and can also be used to study DAG-dependent activation of TRPL channels in Drosophila as well as the photocapacitive effect resulting from membrane-bound photoisomerization.

OptoBI-1 is a photochromic, TRPC3/6/7-selective agonist based on a benzimidazole structure, with an EC₅₀ of approximately 0.1 μM for TRPC3 in its active cis conformation. OptoBI-1 can precisely regulate neuronal firing and calcium signaling in endothelial cells, and can be used to study TRPC6-dependent NFAT signaling pathways in mast cells.

TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 |Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136255 PMID:26317356

Flufenamic Acid-D4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg/kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

L687 is an effective activator of TRPC3/C6/C7, inducing cellular uptake of oligonucleotides.