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.

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.

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).

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.

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

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

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

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.

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.

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.

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.

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

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.

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

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

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).

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

(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.

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.

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.

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.

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

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

Ononetin (2',4'-Dihydroxy-2-(4-methoxyphenyl)acetophenone) is a TRPM3 channel blocker(IC50: 0.3 μM).

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).

M084 (N-Butyl-1H-benzimidazol-2-amine) is a blocker of TRPC4/5 channel, with antidepressant and anxiolytic effects.

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).

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

trans-Dihydromorin is an effective hypopigmenting agent in normal skin cells, hypopigmenting agents effective in melanoma system may not be effective on normal melanocytes, indicating that a non-tumor melanocyte system is more suitable for the screening o

RN-1747 is a selective transient receptor potential cation channel subfamily V member 4 agonists (EC50: 0.77 μM, 4.0 μM, and 4.1 μM for hTRPV4, mTRPV4, and rTRPV4 respectively). RN-1747 also antagonizes TRPM8 (IC50: 4 μM).

TRPA1-IN-2 is a potent and orally active TRPA1 inhibitor with an IC50 value of 0.04 µM.TRPA1-IN-2 has anti-inflammatory activity.

AM-0902 is a potent and specific TRPA1 antagonist (IC50s: 71/131 nM for rTRPA1 and hTRPA1).

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.

D-GsMTx4 TFA, a selective spider venom peptide, is a TRPC1/6 and Piezo2 inhibitor that inhibits cation-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families, blocks cation-selective stretch-activated channels (SACs), and attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglia reactivity. toxicity and microglia reactivity.D-GsMTx4 TFA prevented myocardial infarction in a mouse model of ischemia/reperfusion and can be used to characterize the role of excitatory MSCs in normal physiology and pathology.

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM)

Linopirdine (DuP 996) is a TRPV1 agonist. Linopirdine is an orally active and selective M-type K+ current (IM; Kv7; KCNQ Channels) inhibitor (IC50: 2.4 μM). Linopirdine is a cognitive enhancer. It acts by stimulating release of acetylcholine and other neurotransmitters.Linopirdine is a putative cognition-enhancing drug that increases acetylcholine release in rat brain tissue.

GFB-8438 is a potent and subtype selective inhibitor of TRPC5(IC50s of 0.18 and 0.29 μM of hTRPC5 and hTRPC4, respectively).

SB-366791 is a new and selective cinnamide TRPV1 antagonist.

BCTC is a potent TRPV1 antagonist that inhibits capsaicin-induced and acid-induced activation of rat TRPV1 (IC50 of 35 and 6 nM, respectively)