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TRP/TRPV Channel

TRPV is a family of transient receptor potential cation channels (TRP channels) in animals. All TRPVs are highly calcium selective. TRP channels are a large group of ion channels consisting of six protein families, located mostly on the plasma membrane of numerous human and animal cell types, and in some fungi.

  • Amiloride hydrochloride
    T01752016-88-8
    Amiloride hydrochloride (Amiloride HCl) is an effective sodium channel blocker of epithelial.
    • $15
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  • 1,4-Cineole
    TQ0001470-67-7
    1,4-Cineole (Isocineole) is a natural, oxygenated monoterpene. 1,4-Cineole can activate both human TRPM8 and human TRPA1.
    • $41
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  • Camphor
    T295276-22-2
    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.
    • $29
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  • HC067047 Hydrochloride(883031-03-6 free base)
    T4680L1481646-76-7
    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.
    • $133
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  • OMDM-5
    T12306616884-66-3
    OMDM-5 is a selective anandamide cellular uptake (ACU)inhibitor(Ki of 4.8 μM).
    • $148
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  • AMG-0347
    T29968946615-43-6In house
    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.
    • $397
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  • N4-benzyl-N2-methylquinazoline-2,4-diamine hydrochloride
    T85651135272-09-1
    N4-benzyl-N2-methylquinazoline-2,4-diamine hydrochloride is an inhibitor of TRPC4.
    • $133
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  • OMDM-6
    T12307616884-67-4In house
    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.
    • $195
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  • Cis-22a
    T412331819366-84-1In house
    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.
    • $129
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  • RN-1665
    T777231803003-65-7
    RN-1665 is a potent and selective TRPV4 receptor antagonist.
    • $195
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  • ABT 102
    T29522808756-71-0In house
    ABT 102 (CHEMBL398338) is a selective antagonist of transient receptor potential vanilloid 1 (TRPV1) receptor.
    • $195
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  • Palvanil
    TN679169693-13-6
    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.
    • $133
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  • TC-I2000
    T84491159996-20-9
    TC-I2000 is an TRPM8 channel blocker. Inhibits icilin-induced TRPM8 channel activation in rTRPM8-expressing CHO cells with IC50 of 53 nM.
    • $50
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  • Pinokalant
    T70540149759-26-2In house
    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.
    • $195
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  • MK-2295
    T33429878811-00-8In house
    MK-2295 is a potent TRPV1 antagonist. MK-2295 can be used in studies about the treatment of chronic pain.
    • $117
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  • LASSBio-1135
    T8440852453-71-5
    LASSBio-1135 is an orally effective antagonist of TRPV1 and inhibitor of TNF-α production.
    • $133
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  • (S)-ABT 102
    T29522L808756-70-9In house
    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.
    • $117
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  • NGD-8243
    T9818573678-04-3
    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.
    • $195
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  • A 425619
    T8562581809-67-8
    A 425619 (1-(4-(TRIFLUOROMETHYL)BENZYL)-3-(ISOQUINOLIN-5-YL)UREA) is a potent TRPV1 antagonist
    • $133
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  • 5-(N,N-Hexamethylene)-amiloride
    T46991428-95-1In house
    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.
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    • ABT-239
      T14087460746-46-7In house
      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.
      • $40
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    • JT010
      T15628917562-33-5In house
      JT010 is an effective agonist of TRPA1 (EC50 = 0.65 nM).
      • $32
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    • AP 18
      T2154355224-94-7In house
      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).
      • $30
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    • Oleoyl Serotonin
      T221241002100-44-8In house
      Oleoyl Serotonin is an antagonist of hTRPV1 with an IC50 of 2.57 μM.
      • $59
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    • D-3263 hydrochloride
      T10929L1008763-54-9In house
      D-3263 hydrochloride (D3263 HCl salt) is enteric-coated, orally bioavailable transient receptor potential melatonin member 8 (TRPM8) agonist.
      • $43
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    • Vocacapsaicin hydrochloride
      T393491931116-92-5
      Vocacapsaicin hydrochloride (CA-008 hydrochloride) is a non-opioid TRPV1 agonist, a raw material for capsaicin, and is used for pain relief.
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    • (E)-Cardamonin
      T299419309-14-9
      (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.
      • $30
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    • Rosiglitazone
      T0334122320-73-4
      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.
      • $33
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    • Nonivamide
      T13212444-46-4
      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.
      • $50
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    • HC-030031
      T6530349085-38-7
      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.
      • $46
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    • ML-SA1
      T23004332382-54-4
      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].
      • $47
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    • Capsaicin
      T1062404-86-4
      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.
      • $50
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    • GSK1016790A
      T6848942206-85-1
      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.
      • $31
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    • Diphenyleneiodonium chloride
      T71914673-26-1
      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.
      • $38
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    • EIPA
      TQ01571154-25-2
      EIPA (L593754) (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.
      • $30
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    • AMG 517
      T6379659730-32-2
      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.
      • $47
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    • Englerin A
      T384841094250-15-3
      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.
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    • Caffeic Acid
      T2807331-39-5
      Caffeic Acid is an orally bioavailable, hydroxycinnamic acid derivative and polyphenol, with potential anti-oxidant, anti-inflammatory, and antineoplastic activities.
      • $33
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    • Capsazepine
      T7177138977-28-3
      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.
      • $48
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    • N-(p-amylcinnamoyl) Anthranilic Acid
      T5454110683-10-8
      N-(p-amylcinnamoyl) Anthranilic Acid (ACA) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker.
      • $39
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    • ICILIN
      T181436945-98-9
      ICILIN (AG-3-5) is a synthetic TRPM8 ion channel super-agonist.
      • $31
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    • Dihydrocapsaicin
      T216319408-84-5
      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.
      • $48
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    • SB-705498
      T6660501951-42-4
      SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.
      • $30
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    • Probenecid
      T045757-66-9
      Probenecid (Benemid) is a benzoic acid derivative with antihyperuricemic property.
      • $37
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    • SKF-96365 hydrochloride
      T2170130495-35-1
      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.
      • $52
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    • 2-Aminoethyl diphenylborinate
      T4693524-95-8
      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).
      • $38
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    • HC-067047
      T4680883031-03-6
      HC-067047 is a potent and selective TRPV4 antagonist.Also inhibits the endogenous TRPV4-mediated response to 4α-PDH .
      • $30
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    • Evifacotrep
      T400422413739-88-3
      Evifacotrep is a short transient receptor potential channel 5 ( TRPC5 ) antagonist (WO2020061162, compound 100). Evifacotrep can be used for the research of neurological diseases.
      • $97
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    • JNJ-17203212
      T7526821768-06-3
      JNJ-17203212 is a potent and selective antagonist of TRPV1 (human TRPV1 and rat TRPV1, IC50 of 65 nM and 102 nM).
      • $39
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    • JC-229
      T77645
      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).
      • $30
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