TRP/TRPV Channel

Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.

1,4-Cineole (Isocineole) is a natural, oxygenated monoterpene. 1,4-Cineole can activate both human TRPM8 and human TRPA1.

Camphor (2-Camphanone) is a bicyclic monoterpene ketone found widely in plants, especially CINNAMOMUM CAMPHORA. It is used topically as a skin antipruritic and as an anti-infective agent.

HC-067047 hydrochloride is a potent and selective TRPV4 antagonist. HC-067047 hydrochloride reversibly inhibited currents through the human, rat, and mouse TRPV4 orthologs with IC50 values of 486 nM, 133nM, and 17 nM, respectively.

N4-benzyl-N2-methylquinazoline-2,4-diamine hydrochloride is an inhibitor of TRPC4.

OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).

AMG-0347 (UNII-CD7L9290QR) is a small molecule inhibitor targeting TRPA1(transient receptor potential ankyrin 1) ion channels, a receptor found in sensory neurons and involved in the detection of pain and environmental stimuli. AMG-0347 acts by blocking the function of TRPA1 and has analgesic effects.

Cis-22a is a TRPV6 inhibitor (IC50 = 0.32 μM), which exhibits selectivity against related TRPV channels and calcium channels. cis-22a displays antiproliferative effects on T47D human breast cancer cells.

OMDM-6 is a dual agonist of TRPV1(EC50 = 75 nM) and CB1 (Ki = 3.2 μM). OMDM-6 inhibits anandamide cellular uptake with a Ki of 7.0 μM.

ABT 102 (CHEMBL398338) is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptor.

Palvanil (Hexadecanamide) is a fast desensitizing agonist of TRPV1. it may be promising agents in the therapy of IBS since it modulates intestinal motility and reduces visceral pain.

TC-I2000 is an TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells with IC50 of 53 nM.

Pinokalant (LOE-908) is a novel non-selective cation channel inhibitor.Pinokalant significantly reduces cortical infarct volume in in vivo experiments, improves the metabolic and electrophysiological status of the ischemic penumbra region, and reduces the size of the lesion on magnetic resonance images in the acute phase after middle cerebral artery occlusion in rats.Pinokalant is a potential SARS-CoV-2 protease inhibitor for the study of stroke.

RN-1665 is a potent and selective TRPV4 receptor antagonist.

MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.

N-[(1S)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea is a potent TRPV1 antagonist, blocking activation of TRPV1 by capsaicin with the IC50 of 123 nM.

NGD-8243 (N-[4-(trifluoromethyl)phenyl]-7-[3-(trifluoromethyl)pyridin-2-yl]quinazolin-4-amine) is a TRPV1 inhibitor and can be used in studies for prevention and treatment of cardiac hypertrophy.

A 425619 (1-(4-(TRIFLUOROMETHYL)BENZYL)-3-(ISOQUINOLIN-5-YL)UREA) is a potent TRPV1 antagonist

LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.

5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative, shown to inhibit TRPA1-mediated calcium signal (IC50: 35 μM). It is an inhibitor of the Na+/H+ exchanger (NHE), with Ki of 0.013-2.4 μM for various NHE isoforms. 5-HMA also blocks ASIC3 channels by 51% at 20 μM.

ABT-239 is a novel, highly efficacious antagonist belonging to the non-imidazole class of histamine H3 receptor (H3R) antagonists. It also acts as a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.

Oleoyl Serotonin is an antagonist of hTRPV1 with an IC50 of 2.57 μM.

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

JT010 is an effective agonist of TRPA1 (EC50 = 0.65 nM).

Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.

HC-030031 (TOSLAB 829227) is a potent TRPA1 inhibitor, which antagonizes AITC- and formalin-evoked calcium influx with IC50s of 6.2±0.2 and 5.3±0.2 μM, respectively.

ML-SA1 (Mucolipin synthetic agonist 1) is a selective TRPML agonist, inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 value of ML-SA1 against DENV2 RNA and ZIKV RNA is 8.3 μM and 52.99 μM, respectively[1].

(E)-Cardamonin (Alpinetin chalcone) is a chalconoid that has been isolated from several plants including Alpinia katsumadai and Alpinia conchigera. It is a novel antagonist of hTRPA1 cation channel with an IC50 of 454 nM. It has received growing attention from the scientific community due to the expectations toward its benefits to human health.

Nonivamide (Nonanoic acid vanillylamide) is found in herbs and spices. Nonivamide is an alkaloid from Capsicum species Nonivamide is a flavoring ingredient. Nonivamide is an organic compound and a capsaicinoid. It is an amide of pelargonic acid and vanillylamine. It is present in chili peppers, but is commonly manufactured synthetically. It is more heat-stable than capsaicin.

Rosiglitazone (BRL49653) is a PPARγ agonist, TRPC5 activator, and TRPM3 inhibitor with oral activity. Rosiglitazone is also a hypoglycemic agent and a thiazolidinedione insulin sensitizer.

EIPA (L593754) (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.

Diphenyleneiodonium chloride (DPI)(DPI) is an irreversible inhibitor of iNOS and eNOS (IC50 values of 50 nM and 0.3 μM, respectively),and displays broad-spectrum bactericidal activity.

GSK1016790A (GSK101) (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34 nM in choroid plexus epithelial cells.

Capsaicin ((E)-Capsaicin) is a natural product extracted from Capsicum annuum, and is a TRPV1 agonist (EC50=0.29 μM). Capsaicin has antitumor, anti-inflammatory, antioxidant and neuroprotective activities.

Englerin A, a TRPC4 and TRPC5 channel agonist, is a compound from the East African plant Phyllanthus engleri with analgesic, anti-inflammatory, and anticancer activities that induces necrosis in human renal cancer cells.

AMG 517 is an effective and specific TRPV1 antagonist, antagonizes proton (IC50: 0.76 nM), capsaicin (IC50: 0.62 nM), and heat activation (IC50: 1.3 nM) of TRPV1.

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM). Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. It is therefore considered to be a capsaicin antagonist.

Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.

ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.

Dihydrocapsaicin (CCRIS1589) is isolated from Capsicum fruit. Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Like capsaicin, dihydrocapsaicin is an irritant. Capsaicin is found in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain pure dihydrocapsaicin. Dihydrocapsaicin represents about 10% of the compound present in commercial preparations purporting to be pure capsaicin, but it has about the same pungency as capsaicin. VR1 (vanilloid receptor 1) is a heat activated calcium ion channel which functions as a part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. The potency of dihydrocapsaicin at VR1 appears equivalent to capsaicin. Antioxidant. Reduces oxidation of serum lipids. Mutagenic. Dihydrocapsaicin is an activator of VR1.

SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.

Probenecid (Benemid) is a benzoic acid derivative with antihyperuricemic property.

N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker.

HC-067047 is a potent and selective TRPV4 antagonist.Also inhibits the endogenous TRPV4-mediated response to 4α-PDH .

2-Aminoethyl diphenylborinate (2-APB) is a chemical that acts to inhibit both IP3 receptors and TRP channels (although it activates TRPV1, TRPV2, & TRPV3 at higher concentrations).

SKF-96365 hydrochloride (SKF96365) , a SOCE inhibitor, exhibits potent anti-neoplastic activity by inducing cell-cycle arrest and apoptosis in colorectal Y cells. SKF-96365 hydrochloride can induce cytoprotective autophagy to delay apoptosis by preventing the release of cytochrome c (cyt c) from the mitochondria into the cytoplasm. Mechanistically, SKF-96365 hydrochloride treatment inhibited the calcium calmodulin-dependent protein kinase IIγ (CaMKIIγ) AKT signaling cascade in vitro and in vivo. Overexpression of CaMKIIγ or AKT abolished the effects of SKF-96365 on Y cells, suggesting a critical role of the CaMKIIγ AKT signaling pathway in SFK-96365-induced biological effects. SKF-96365 hydrochloride inhibited hERG current in a concentration-dependent manner.

JC-229 is a potent and selective TbRPA1 inhibitor that can inhibit RPA1 in Trypanosoma brucei. JC-229 can be used to study human African Trypanosomiasis (HAT).

Evifacotrep is a short transient receptor potential channel 5 ( TRPC5 ) antagonist (WO2020061162, compound 100). Evifacotrep can be used for the research of neurological diseases.

JNJ-17203212 is a potent and selective antagonist of TRPV1 (human TRPV1 and rat TRPV1, IC50 of 65 nM and 102 nM).