Catalog No.
Product Name
Application
Product Information
Citations
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TRPC1/4/5 channels inhibitor
Pico145 is a remarkable inhibitor of TRPC1/4/5 channels, inhibits (?)-englerin A-activated TRPC4/TRPC5 channels, with IC50s of 0.349 and 1.3 nM in cells, and shows no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8.- Aki Teranishi, .et al. , Nat Commun, 2024, Dec 12;15(1):10476 PMID: 39668169
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TRPC3 inhibitor
Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(9):1444-1455 PMID: 41033978
- Keisuke Obara, .et al. , Biol Pharm Bull, 2025, 48(6):932-940 PMID: 40582844
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TRPA1 channel blocker
A 967079 is a selective TRPA1 channel blocker (IC50 values are 67 and 289 nM at human and rat TRPA1 receptors respectively).- L Jin, Z Xie, .et al. , Am J Physiol Heart Circ Physiol, 2023, Dec 1;325(6):H1446-H1460 PMID: 37889254
- L Jin, .et al. , Toxicol Appl Pharmacol, 2021, Jul 13;426:115647 PMID: 34271065
- L. Jin, .et al. , Toxicology and Applied Pharmacology, 2020, 398(1), PMID: 32320793
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MSCs Inhibitor
GsMTX4 is a 34 amino acid peptidyl toxin isolated from the Grammostola rosea (Chilean rose) tarantula venom and belongs to the huwentoxin-1 family.- Shota Inoue, .et al. , Bone, 2023, Dec:177:116916 PMID: 37777037
- Jean-Baptiste Cavin, .et al. , J Physiol, 2023, Apr;601(7):1183-1206 PMID: 36752210
- Yong Chen, .et al. , Gastroenterology, 2021, Apr 2 PMID: 33819485
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TRPV1 antagonist
AMG 517 is a potent and selective TRPV1 antagonist.- Thieu X Phan, .et al. , J Physiol, 2022, Apr;600(7):1651-1666 PMID: 35020949
- Jun Hai, .et al. , Biosci Biotechnol Biochem, 2020, Jul 7;1-7 PMID: 32633621
- Hai J, .et al. , Biomed Res, 2018, 39(6):279-286 PMID: 30531157
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TRPC6 inhibitor
TRPC6-IN-1 is a Transient Receptor Potential Canonical 6 Channel (TRPC6) inhibitor, with an EC50 of 4.66 μM. -
TRPV1 antagonist
NJ-17203212 is a novel and selective TRPV1 antagonist, with IC50 of 65 nM and 102 nM for human TRPV1 and rat TRPV1. -
TrpA1 channel agonist
PF-4840154 is a non-electrophilic reference agonist of the TrpA1 channel. The TRPA1 channel is considered an attractive pain target based on the fact that TRPA1 knockout mice showed near complete attenuation of pain behaviors in some pre-clinical development models. -
TRPA1 channel blocker
TCS 5861528 is a TRPA1 channel blocker and an antagonizer of AITC- and 4-HNE-evoked calcium influx. -
TRPV4 blocker
GSK2193874 was identified as a selective, orally active TRPV4 blocker that inhibits Ca(2+) influx through recombinant TRPV4 channels and native endothelial TRPV4 currents. -
TRPC6 inhibitor
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels that opens new opportunities for the investigation of TRPC channel function in vivo. SAR7334 inhibited TRPC6, TRPC3 and TRPC7-mediated Ca(2+) influx into cells with IC50 s of 9.5, 282 and 226 nM, whereas TRPC4 and TRPC5-mediated Ca(2+) entry was not affected. - Nonivamide is a capsaicin analogue that exhibits anti-inflammatory properties in peripheral blood mononuclear cells and U-937 macrophages. Nonivamide is a agonist, which exhibits 4d-EC50 value of 5.1 mg/L in static toxicity tests.
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TRPM4 blocker
Selective TRPM4 blocker (IC50 = 20 μM in HEK293 cells). Exhibits no effect on CFTR or TRPM5 (at 0.25 and 1 mM respectively). Abolishes arrhythmias induced by hypoxia in a mouse heart model. -
TRPV1 agonist
Zucapsaicin, also known as cis-Capsaicin, is a medication used to treat osteoarthritis of the knee and other neuropathic pain. It is applied three times daily for a maximum of three months. It reduces pain, and improves articular functions. -
TRPM8 antagonist
RQ-00203078 is a highly selective, potent and orally available TRPM8 antagonist (IC50 values are 5.3 and 8.3 nM for rat and human channels respectively), exhibits >350-fold selectivity for TRPM8 over TRPV4, TRPV1 and TRPA1. -
TRPV4 Activator
GSK1016790A is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells. - Camphor is a waxy, flammable, white or transparent solid with a strong aroma, often used to relieve pain, reduce itching and treat fungal infections. It can activate TRPV1 and TRPV3
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Calcium Channel /TRP5 antagonist
Lomerizine dihydrochloride is a antagonist at L-type and T-type Ca 2+ channels and TRp5 channels used to treat migraines and vertigo. -
TRP Channel blocker
SKF-96365 hydrochloride is a non-selective TRP Channel blocker. -
TRPV4 ion channel blocker
GSK2798745 is a first-in-class, highly potent, selective, orally active transient receptor potential vanilloid 4 (TRPV4) ion channel blocker with IC50s of 1.8 and 1.6 nM for hTRPV4 and rTRPV4, respectively. -
TRPV1 receptor antagonist
Capsazepine is a synthetic analogue of the sensory neurone excitotoxin, and an antagonist of TRPV1 receptor with an IC50 of 562 nM. -
TRPP3 channel inhibitor
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. EIPA also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
