Home Transmembrane Transporters TRP Channel

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.
Exp Lung Res, 2025, 51(1):23-37
J Vis Exp, 2025, (224)
Research Square, 2024, 10.21203/rs.3.rs-3863076/v1
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
Mol Pain, 2023, 19:17448069231158290
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.
J Adv Res, 2025, S2090-1232(25)00267-X
J Nanobiotechnology, 2025, 23(1):173
iScience, 2025, 28(2):111830
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
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
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
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
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
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.
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.