TRP Channel Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Cell Death Discov, 2025, 11(1):449
Exp Lung Res, 2025, 51(1):23-37
J Vis Exp, 2025, (224)
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
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
Lipids in Health and Disease, 2023, 6
S9849 EIPA (L593754) EIPA (L593754; MH 12-43) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.
MedComm (2020), 2026, 7(3):e70657
J Adv Res, 2025, S2090-1232(25)00267-X
J Nanobiotechnology, 2025, 23(1):173
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.

Journal of Biological Chemistry, 2025, 110716
J Biol Chem, 2025, 301(10):110716
bioRxiv, 2025, 2025.06.11.659112
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
Verified customer review of Caffeic Acid
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
ProQuest, 2021, 28432832
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
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.
Antioxidants (Basel), 2025, 15(1)38
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.
Endocrinology, 2022 Jul 1, bqac081
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.
Brain, 2017, 669-683
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
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
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.
S9932New GSK2798745 GSK2798745 is a potent, selective, orally active TRPV4 ion-channel blocker, with IC50 values of 1.8 nM at human TRPV4 and 1.6 nM at rat TRPV4. It exhibits the potential to be used in research compound in cardiac and respiratory disease studies, including research related to heart-failure-associated pulmonary edema.