trpc5

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

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

AM12 inhibits lanthanide-evoked TRPC5 activity (IC50: 0.28 μM).

HC-070 is a TRPC5 and TRPC4 antagonist (IC50 = 9.3 nM and 46 nM).

Pico145 (HC-608) is a remarkable inhibitor of TRPC1/4/5 channels, specifically inhibiting ( )-englerin A-activated TRPC4/TRPC5 channels with IC50s of 0.349 and 1.3 nM in cells, while showing no effect on TRPC3, TRPC6, TRPV1, TRPV4, TRPA1, TRPM2, or TRPM8.

Clemizole hydrochloride is an antagonist for H1 histamine receptor. According to the research, Clemizole hydrochloride can inhibit hepatitis C virus (HCV) replication and NS4B's RNA binding.

ML204 is a novel potent antagonist that selectively modulates native TRPC4/C5 ion channels.

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.

Evifacotrep is a short transient receptor potential channel 5 ( TRPC5 ) antagonist (WO2020061162, compound 100). Evifacotrep can be used for the research of neurological diseases.

AC1903 is a specific inhibitor of TRPC5 channel, and has been shown to suppress severe proteinuria and prevent podocyte loss.

TRPC5-IN-5 (Compound ph8) is a TRPC5 inhibitor with an IC50 value of 1.28 μM. It is applicable in research related to neurological and kidney diseases.

TRPC5-IN-1 is a TRPC5 inhibitor active in various animal models of chronic kidney disease.

TRPC5-IN-3 is a potent TRPC5 inhibitor with an IC50 of 10.75 nM.

TRPC5-IN-2 is a potent inhibitor of TRPC5.

TRPC5 modulator-1 (Compound 9) is a TRPC5 modulator with an IC50 of less than 1 nM, suitable for studying neuropsychiatric disorders.

TRPC5-IN-4, a potent and safe TRPC inhibitor, exhibits IC50 values of 14.07 nM and 65 nM for TRPC5 and TRPC4, respectively, indicating high efficacy. It does not cause damage to liver and kidney cellular components, making it suitable for chronic kidney disease (CKD) research [1].

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.

Rosiglitazone hydrochloride (BRL-49653 HCl) is a blood glucose-lowering drugs, stimulating insulin secretion by binding to the PPAR receptors in fat cells.

Rosiglitazone maleate (BRL 49653) is the maleate salt of rosiglitazone, an orally-active thiazolidinedione with antidiabetic properties and potential antineoplastic activity.

Rosiglitazone sodium is an effective and selective PPARγ activator, with EC50 values of 30 nM for PPARγ1, 100 nM for PPARγ2, and 60 nM for PPARγ. It also has an approximate Kd of 40 nM for PPARγ. Additionally, Rosiglitazone sodium acts as a regulator of TRP channels, inhibiting the activities of TRPM2 and TRPM3, while activating TRPC5.

TRPC4 5-IN-3 (Compound 32) is an orally active inhibitor of transient receptor potential canonical channels 4 and 5 (TRPC4 5), with IC50 values of 3.6 nM and 5.5 nM, respectively. It inhibits the hERG channel with an IC50 of 6.5 µM. This compound demonstrates good metabolic stability in human, rat, and mouse liver microsomes. In mouse models, TRPC4 5-IN-3 exhibits antidepressant and anxiolytic effects and displays favorable pharmacokinetic properties, with an oral bioavailability of 87%.

TRPC6 antagonist-1 (X26) is a TRPC6 inhibitor with IC50 values of 0.97 μM for TRPC6, 3.93 μM for TRPC3, 5.77 μM for TRPC5, and 4.37 μM for TRPC7. Additionally, TRPC6 antagonist-1 hinders TGF-β1-induced myofibroblast differentiation, thereby mitigating renal fibrosis.

TRPC antagonist1 (compound 15g) is a potent TRP channel (TRPC) antagonist with IC50 values of 2.4 μM, 12.2 μM, 7.6 μM, 2.9 μM, and 3.4 μM for TRPC3, TRPC4, TRPC5, TRPC6, and TRPC7, respectively. It demonstrates significant anti-glioblastoma efficacy in vitro against the U87 cell line.

TRPC4/5-IN-2 (Compound 12) is an orally active transient receptor potential (TRPC5) inhibitor with an IC50 value of 81 nM. This compound exhibits good biosafety and low hepatic and renal toxicity, making it a promising candidate for the treatment of chronic kidney disease (CKD).