| S2556 |
Rosiglitazone
|
Rosiglitazone is a potent antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively. This compound is a pure ligand of PPAR-gamma, and has no PPAR-alpha-binding action. It modulates TRP channels and induces autophagy. It also prevents ferroptosis. |
-
Nat Commun, 2025, 16(1):6241
-
Lab Invest, 2025, 105(4):104103
-
Nat Commun, 2024, 15(1):1429
|
|
| S8639 |
DPI (Diphenyleneiodonium chloride)
|
DPI (Diphenyleneiodonium chloride) is an inhibitor of NADPH oxidase and also a potent, irreversible, and time-, temperature-dependent iNOS/eNOS inhibitor. It also functions as a TRPA1 activator and selectively inhibits intracellular reactive oxygen species (ROS). |
-
Redox Biol, 2025, 80:103485
-
Sci Adv, 2025, 11(34):eadv6937
-
Exp Mol Med, 2024, 56(12):2602-2616
|
|
| S2505 |
Rosiglitazone maleate
|
Rosiglitazone maleate, a member of the thiazolidinedione class of antihyperglycaemic agents, is a high-affinity selective agonist of the peroxisome proliferator-activated receptor-γ (PPAR-γ) with IC50 of 42 nM. This compound also modulates TRP channels and induces autophagy. It prevents ferroptosis. |
-
Stem Cell Reports, 2022, 17(11):2531-2547
-
Cell Death Dis, 2021, 12(11):972
-
Antioxidants (Basel), 2021, 10(2)155
|
|
| S7999 |
SKF96365
|
SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. |
-
Exp Lung Res, 2025, 51(1):23-37
-
J Vis Exp, 2025, (224)
-
Research Square, 2024, 10.21203/rs.3.rs-3863076/v1
|
|
| S7115 |
AMG-517
|
AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. |
-
Mucosal Immunol, 2024, S1933-0219(24)00006-0
-
Front Immunol, 2024, 15:1477072
-
iScience, 2023, 26(5):106749
|
|
| S2918 |
HC-030031
|
HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. |
-
Int J Mol Sci, 2025, 26(3)1385
-
Lipids Health Dis, 2023, 22(1):6
-
Mol Pain, 2023, 19:17448069231158290
|
|
| S1990 |
Capsaicin(Vanilloid)
|
Capsaicin(Vanilloid) is an active component of chili peppers, which are plants belonging to the genus Capsicum. It is a TRPV1 agonist with an EC50 of 0.29 μM in HEK293 cells. This compound is a mixture of Capsaicin and Dihydrocapsaicin. |
-
J Biomed Sci, 2025, 32(1):47
-
Int J Mol Sci, 2025, 26(1)380
-
Biol Pharm Bull, 2025, 48(6):769-781
|
|
| S6657 |
2-APB (2-Aminoethyl Diphenylborinate)
|
2-Aminoethyl Diphenylborinate (2-APB) is an IP3 receptor inhibitor and regulates IP3-induced calcium release. It also inhibits the SOC channel activity and, at higher concentrations, inhibits TRP channel. |
-
Cell Prolif, 2025, e70120.
-
PLoS Pathog, 2025, 21(1):e1012872
-
Liver Int, 2025, 45(10):e70341
|
|
| S8367 |
GSK2193874
|
GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. |
-
Brain Stimul, 2025, 18(5):1455-1469
-
Int J Oral Sci, 2024, 16(1):3
-
iScience, 2023, 26(5):106749
|
|
| S8137 |
Capsazepine
|
Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
-
Biol Pharm Bull, 2025, 48(6):769-781
-
J Ethnopharmacol, 2024, 337(Pt 2):118882
-
Sci Adv, 2023, 9(27):eadg9593
|
|
| S8107 |
GSK1016790A
|
GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells. |
-
Brain Stimul, 2025, 18(5):1455-1469
-
Am J Physiol Lung Cell Mol Physiol, 2024, 326(3):L252-L265
-
iScience, 2023, 26(5):106749
|
|
| S2773 |
SB705498
|
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. |
-
Oxid Med Cell Longev, 2022, 2022:8096009
-
IUBMB Life, 2022, 10.1002/iub.2605
-
Biogerontology, 2016, 17(5-6):907-920
|
|
| S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO). |
-
Molecules, 2021, 26(5)1210
-
J Nutr Biochem, 2015, 26(11):1379-84
-
Sci Rep, 2015, 5:12580
|
|
| S4022 |
Probenecid
|
Probenecid (Benemid) is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. This compound is also a clinically used broad-spectrum Pannexin1 (Panx1) blocker. |
-
BMC Vet Res, 2025, 21(1):237
-
Mil Med Res, 2024, 11(1):41
-
Front Immunol, 2022, 13:992505
|
|
| S6637 |
HC-067047
|
HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. |
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-01008-7
-
Cell Physiol Biochem, 2024, 58(4):292-310
-
Front Pharmacol, 2023, 14:1101498
|
|
| S2650 |
RN-1734
|
RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. This compound alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells. |
-
Theranostics, 2022, 12(4): 1621-1638
-
Theranostics, 2022, 12(4):1621-1638
|
|
| S3942 |
Cardamonin
|
Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while this compound does not interact with TRPV1 nor TRPV4 channel. |
-
Cell, 2023, 186(13):2929-2949.e20
-
Food Funct, 2021, 12(23):11808-11818
|
|
| S8691 |
ML204
|
ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels. |
-
Nature, 2019, 567(7747):262-266
|
|
| S8238 |
SB366791
|
SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM. |
-
Mol Pain, 2018, 14:1744806918816850
|
|
| S4714 |
(-)-Menthol
|
(-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8. |
-
Curr Biol, 2019, 29(11):1787-1799.e5
|
|
| F2784New |
TRPC1 Antibody [J16G9]
|
|
|
|
| F2619New |
TRPM7 + TRPM6 Antibody [N14M16]
|
|
|
|
| S6122 |
Cyclohexanecarboxamide
|
Cyclohexanecarboxamide (Ethyl menthane carboxamide, WS3, Hexahydrobenzamide) is a cooling agent and an agonist at TRPM8 receptors (EC50 = 3.7 μM). |
|
|
| S6638 |
AMG-333
|
AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8. |
|
|
| E5869New |
ML-SA5
|
ML-SA5 is a potent agonist of TRPML1 cation channel that activates the entire endosomal TRPML1 (ML1) current in DMD myocytes with an EC50 of 285 nM and exhibit anticancer activity. |
|
|
| E1890New |
A-967079
|
A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. This compound decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS). |
|
|
| S6947 |
MK6-83
|
MK6-83 is a novel Transient receptor potential melastatin member 1 (TRPML1) activator that may be used as a potential pharmacological treatment option for a specific subgroup of MLIV patients. |
|
|
| E4659 |
Pyr3
|
Pyr3 is a selective and potent inhibitor of transient receptor potential canonical channel 3 (TRPC3). It inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 0.7 μM. It holds potential for treating TRPC3-related diseases like cardiac hypertrophy. |
|
|
| S0825 |
MDR-652
|
MDR-652 is a potent and specific agonist of transient receptor potential vanilloid 1 (TRPV1) with Ki of 11.4 nM and 23.8 nM for hTRPV1 and rTRPV1, respectively. This compound has excellent and dose-dependent analgesic activity. |
|
|
| S8073 |
Optovin
|
Optovin is a reversible photoactivated TRPA1 activator.
|
-
Cancer Drug Resist, 2025, 8:45
|
|
| S9140 |
Pulegone
|
Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient.pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations. |
|
|
| S0750 |
GFB-8438
|
GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel. |
|
|
| E5813New |
JNJ-28583113
|
JNJ-28583113 is a potent, brain-penetrant antagonist of TRPM2 with an IC50 of 126 nM that protects cells from oxidative stress-induced death and morphological changes. It also inhibits microglial cytokine release in response to pro-inflammatory stimuli and promotes GSK3α/β phosphorylation. |
|
|
| S0977 |
AC1903
|
AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM. |
-
Front Med (Lausanne), 2024, 11:1381479
|
|
| S6634 |
SAR7334
|
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels. This compound blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. |
-
Adv Healthc Mater, 2025, e2404767.
-
Nat Commun, 2024, 15(1):10476
|
|
| S7848 |
QX-314 chloride
|
QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels. |
|
|
| E2871 |
Trovafloxacin Mesylate
|
Trovafloxacin mesylate, a broad-spectrum quinolone antibiotic, is a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. |
|
|
| E2515 |
JT010
|
JT010 is a potent agonist of transient receptor potential cation channel subfamily A member 1 (TRPA1) with an EC50 of 0.65 nM. |
|
|
| S3756 |
Methyl salicylate
|
Methyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
|
|
| S3763 |
Cinnamaldehyde
|
Cinnamaldehyde is a flavonoid that is naturally synthesized by the shikimate pathway. Its supplementation can improve glucose and lipid homeostasis in diabetic animals; a TRPA1 agonist. |
-
Bioact Mater, 2025, 43:240-254
-
Int J Mol Sci, 2023, 24(11)9501
-
Int J Mol Sci, 2023, 24(11)9501
|
|
| S6934 |
AMG-9810
|
AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. This compound blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. It significantly reduces the mRNA expression of TLR2 and TLR4. This chemical also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling. |
-
Int J Mol Sci, 2025, 26(18)8816
|
|
| S6838 |
BCTC
|
BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. This compound inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. It exhibits anti-tumor activity. |
|
|
| S6409 |
Zucapsaicin
|
Zucapsaicin, the cis-isomer of capsaicin, is a topical analgesic used to treat osteoarthritis of the knee and other neuropathic pain. It is also a TRPV-1 modulator. |
-
Arch Biochem Biophys, 2024, 754:109958
|
|
| S6070 |
CBA (TRPM4-IN-5)
|
CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM. |
|
|
| S6410 |
Clemizole
|
Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. |
|
|
| S9086 |
Dihydrocapsaicin
|
Dihydrocapsiacin (6,7-Dihydrocapsaicin, 8-Methyl-N-vanillylnonanamide, CCRIS1589), found in pepper (C. annuum), is a potential nutriceutical. This compound is a selective TRPV1 agonist. |
|
|
| S0174 |
TRPM8 antagonist 2
|
TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes. |
|
|
| E0028 |
9-Phenanthrol
|
9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.
|
-
Theranostics, 2025, 15(14):6901-6918
|
|
| E0031 |
RN-1747
|
RN-1747 is a selective TRPV4 agonist with EC50s of 0.77 μM, 4.0 μM and 4.1 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. This compound also antagonizes TRPM8 with IC50 of 4 μM. |
|
|
| E0026 |
ML-SI3
|
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
|
-
J Biol Chem, 2025, 301(10):110716
-
bioRxiv, 2025, 2025.06.11.659112
-
Sci Rep, 2024, 14(1):24836
|
|
| S9926 |
ML-SA1
|
ML-SA1 (Mucolipin synthetic agonist 1) is an activator of TRPML channels. This compound also inhibits Dengue virus 2 (DENV2) and Zika virus (ZIKV) by promoting lysosomal acidification and protease activity. The IC50 values of this chemical against DENV2 RNA and ZIKV RNA are 8.93 μM and 52.99 μM, respectively. It induces autophagy. It can be used for the research of broad-spectrum antiviral. |
-
Sci Rep, 2024, 14(1):24836
|
|
| S5419 |
1,4-Cineole
|
1,4-Cineole (Isocineole) is a widely distributed, natural, oxygenated monoterpene. This compound, present in eucalyptus oil, activates both human TRPM8 and human TRPA1. |
|
|
| E2684 |
Icilin
|
Icilin is an agonist of the transient receptor potential M8 (TRPM8) ion channel with an EC50 of 1.4 μM. |
|
|
| E4648 |
Pico145
|
Pico145(HC-608) is a selective inhibitor of TRPC1/4/5 channels. It inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50 values of 0.349 and 1.3 nM, respectively. It exhibits no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
-
Biol Pharm Bull, 2025, 48(9):1444-1455
|
|
| S4787 |
Methyl syringate
|
Methyl syringate (Syringic Acid Methyl Ester), a plant phenolic compound, is a specific and selective TRPA1 agonist. |
|
|
| S3851 |
Camphor
|
Camphor (2-Bornanone, Bornan-2-one, 2-Camphanone, Formosa) is a bicyclic monoterpene ketone found widely in plants, especially cinnamomum camphora and used topically as a skin antipruritic and as an anti-infective agent. |
-
iScience, 2023, 26(5):106749
|
|
| S4516 |
(+)-Camphor
|
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. |
|
|
| S3867 |
(E)-Cardamonin
|
(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-κB inhibitor. |
|
|
| S2963 |
WS-12
|
WS-12 is a potent TRPM8 agonist with an EC50 of 39 nM. |
|
|
| E4673 |
AMTB hydrochloride
|
AMTB hydrochloride is a blocker of the transient receptor potential melastatin 8 (TRPM8) ion channel. It reduces the activation of TRPM8 channels induced by icilin, as assessed through a Ca2+ influx assay, with a pIC50 of 6.23. It is used as a tool to evaluate the role of this channel in bladder rhythmic contraction. |
|
|
| S7999 |
SKF96365
|
SKF96365, originally identified as a blocker of receptor-mediated calcium entry, is widely used diagnostically, as a blocker of transient receptor potential canonical type (TRPC) channels. |
- Exp Lung Res, 2025, 51(1):23-37
- J Vis Exp, 2025, (224)
- Research Square, 2024, 10.21203/rs.3.rs-3863076/v1
|
|
| S2918 |
HC-030031
|
HC-030031 (TOSLAB 829227) is a selective TRPA1 channel blocker that antagonizes AITC- and formalin-evoked calcium influx with IC50 of 6.2 μM and 5.3 μM respectively. |
- Int J Mol Sci, 2025, 26(3)1385
- Lipids Health Dis, 2023, 22(1):6
- Mol Pain, 2023, 19:17448069231158290
|
|
| S8367 |
GSK2193874
|
GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively. |
- Brain Stimul, 2025, 18(5):1455-1469
- Int J Oral Sci, 2024, 16(1):3
- iScience, 2023, 26(5):106749
|
|
| S2277 |
Caffeic Acid
|
Caffeic acid is a hydroxycinnamic acid, a naturally occurring organic compound. Caffeic acid is an inhibitor of both TRPV1 ion channel and 5-Lipoxygenase (5-LO). |
- Molecules, 2021, 26(5)1210
- J Nutr Biochem, 2015, 26(11):1379-84
- Sci Rep, 2015, 5:12580
|
|
| S8691 |
ML204
|
ML204 is a novel, potent, and selective TRPC4 channel inhibitor with apparent IC50 values of about 1 μM in fluorescent intracellular Ca2+ assays and about 3 μM in whole-cell voltage clamp experiments. It exhibits some selectivity within the TRPC subfamily of channels and higher selectivity against other TRP channels and non-TRP channels. |
- Nature, 2019, 567(7747):262-266
|
|
| E4659 |
Pyr3
|
Pyr3 is a selective and potent inhibitor of transient receptor potential canonical channel 3 (TRPC3). It inhibits TRPC3-mediated Ca2+ influx in a dose-dependent manner with the IC50 value of 0.7 μM. It holds potential for treating TRPC3-related diseases like cardiac hypertrophy. |
|
|
| S9140 |
Pulegone
|
Pulegone, a naturally occurring organic compound, is a fragrance and flavour ingredient.pulegone stimulates both TRPM8 and TRPA1 channel in chicken sensory neurons and suppresses the former but not the latter at high concentrations. |
|
|
| S0750 |
GFB-8438
|
GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel. |
|
|
| S0977 |
AC1903
|
AC1903 (compound 2) is a specific and selective TRPC5 (transient receptor potential canonical channel 5) inhibitor with IC50 of 4.06 μM. |
- Front Med (Lausanne), 2024, 11:1381479
|
|
| S6634 |
SAR7334
|
SAR7334 is a novel, highly potent and bioavailable inhibitor of TRPC6 channels. This compound blocks TRPC6 currents with an IC50 of 7.9 nM in patch-clamp experiment. |
- Adv Healthc Mater, 2025, e2404767.
- Nat Commun, 2024, 15(1):10476
|
|
| E2871 |
Trovafloxacin Mesylate
|
Trovafloxacin mesylate, a broad-spectrum quinolone antibiotic, is a potent, selective and orally active pannexin 1 channel (PANX1) inhibitor with an IC50 of 4 μM for PANX1 inward current. |
|
|
| S6070 |
CBA (TRPM4-IN-5)
|
CBA (TRPM4-IN-5, Compound 5) is a highly selective blocker of the TRPM4 ion channel with an IC50 of 1.5μM. |
|
|
| S6410 |
Clemizole
|
Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels. |
|
|
| E0028 |
9-Phenanthrol
|
9-Phenanthrol (9-Hydroxyphenanthrene, Phenanthren-9-o, 9-Phenanthrenol) is a selective TRPM4 inhibitor with an IC50 in the range of 0.02 μM, without effects on TRPM5.
|
- Theranostics, 2025, 15(14):6901-6918
|
|
| E0026 |
ML-SI3
|
ML-SI3 is a potent TRPML channel inhibitor with IC50s of 4.7 µM and 1.7 µM for TRPML1 and TRPML2, respectively.
|
- J Biol Chem, 2025, 301(10):110716
- bioRxiv, 2025, 2025.06.11.659112
- Sci Rep, 2024, 14(1):24836
|
|
| E4648 |
Pico145
|
Pico145(HC-608) is a selective inhibitor of TRPC1/4/5 channels. It inhibits (−)-englerin A-activated TRPC4/TRPC5 channels, with IC50 values of 0.349 and 1.3 nM, respectively. It exhibits no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, TRPM8. |
- Biol Pharm Bull, 2025, 48(9):1444-1455
|
|
| S7115 |
AMG-517
|
AMG 517 is a potent and selective TRPV1 antagonist, and antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM, respectively. |
- Mucosal Immunol, 2024, S1933-0219(24)00006-0
- Front Immunol, 2024, 15:1477072
- iScience, 2023, 26(5):106749
|
|
| S8137 |
Capsazepine
|
Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01. |
- Biol Pharm Bull, 2025, 48(6):769-781
- J Ethnopharmacol, 2024, 337(Pt 2):118882
- Sci Adv, 2023, 9(27):eadg9593
|
|
| S2773 |
SB705498
|
SB705498 is a TRPV1 antagonist for hTRPV1, antagonizes capsaicin, acid, and heat activation of TRPV1 with IC50 of 3 nM, 0.1 nM and 6 nM, shows a degree of voltage dependence, exhibits >100-fold selectivity for TRPV1 over TRPM8. Phase 2. |
- Oxid Med Cell Longev, 2022, 2022:8096009
- IUBMB Life, 2022, 10.1002/iub.2605
- Biogerontology, 2016, 17(5-6):907-920
|
|
| S6637 |
HC-067047
|
HC-067047 is a selective TRPV4 channel antagonist with IC50 values of 48 nM,133 nM,and 17 nM for human, rat, and mouse TRPV4 orthologs,respectively. |
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-01008-7
- Cell Physiol Biochem, 2024, 58(4):292-310
- Front Pharmacol, 2023, 14:1101498
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| S2650 |
RN-1734
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RN-1734 (TRPV4 Antagonist I) is a selective transient receptor potential vanilloid 4 (TRPV4) antagonist with IC50 of 2.3 μM, 5.9 μM and 3.2 μM for hTRPV4, mTRPV4 and rTRPV4, respectively. This compound alleviates demyelination and inhibits glial activation and the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells. |
- Theranostics, 2022, 12(4): 1621-1638
- Theranostics, 2022, 12(4):1621-1638
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| S3942 |
Cardamonin
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Cardamonin (Alpinetin chalcone), isolated from the fruits of Alpinia species, is a chalconoid with anti-inflammatory and anti-tumor activity. It has been shown to be a novel antagonist of hTRPA1 cation channel with IC50 of 454 nM while this compound does not interact with TRPV1 nor TRPV4 channel. |
- Cell, 2023, 186(13):2929-2949.e20
- Food Funct, 2021, 12(23):11808-11818
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| S8238 |
SB366791
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SB-366791 is a novel, potent, and selective, cinnamide TRPV1 antagonist with an IC50 of 5.7 nM. |
- Mol Pain, 2018, 14:1744806918816850
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| S6638 |
AMG-333
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AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8. |
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| E1890New |
A-967079
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A-967079 is a selective antagonist of TRPA1 receptor with IC50 values of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively. This compound decreases the responses of wide dynamic range (WDR), and nociceptive specific (NS) neurons following noxious pinch stimulation and high-intensity mechanical stimulation in rats. It demonstrates strong penetration into the central nervous system (CNS). |
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| E5813New |
JNJ-28583113
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JNJ-28583113 is a potent, brain-penetrant antagonist of TRPM2 with an IC50 of 126 nM that protects cells from oxidative stress-induced death and morphological changes. It also inhibits microglial cytokine release in response to pro-inflammatory stimuli and promotes GSK3α/β phosphorylation. |
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| S3756 |
Methyl salicylate
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Methyl salicylate (Betula oil, Gaultheria oil, Methyl 2-hydroxybenzoate, Natural wintergreen oil) is an organic ester naturally produced by many species of plants, particularly wintergreens. It is an agonist for TRPA1 and TRPV1. |
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| S6934 |
AMG-9810
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AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. This compound blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. It significantly reduces the mRNA expression of TLR2 and TLR4. This chemical also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling. |
- Int J Mol Sci, 2025, 26(18)8816
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| S6838 |
BCTC
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BCTC is an orally effective and highly potent vanilloid receptor 1 (VR1/TRPV1) antagonist. This compound inhibits capsaicin-induced and acid-induced activation of rat VR1 with IC50 of 35 nM and 6.0 nM, respectivley. It exhibits anti-tumor activity. |
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| S0174 |
TRPM8 antagonist 2
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TRPM8 antagonist 2 (TRPM8 Antagonist) is a potent and selective antagonist of TRPM8 with IC50 of 0.2 nM that can be used for the pharmacological treatment of neuropathic pain syndromes. |
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| S3867 |
(E)-Cardamonin
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(E)-Cardamonin (Alpinetin chalcone, cardamomin) is a naturally occurring chalcone with strong anti-inflammatory activity. It is a novel TRPA1 antagonist with IC50 of 454 nM and also a NF-κB inhibitor. |
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