trpc5

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

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

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].

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

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

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

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

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.

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).

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

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

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

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

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.

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-1 can be used for the research of skin inflammatory diseases and proteinuric kidney diseases. TRPC4 5-IN-1 is a potent inhibitor of TRP channel 5 4 (TRPC5 4) with IC50 values of 0.54 μM and 2.06 μM, respectively. [1].

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%.

TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 |Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136255 PMID:26317356

BTD is a selective transient receptor potential classical 5 (TRPC5) activator, which activates heteromeric channel complexes formed by TRPC5 and its recent relatives TRPC1 or TRPC4, used for studying neurodegenerative diseases.

M084 hydrochloride, a TRPC4/5 channel blocker, exhibits IC50 values of 10.3 μM and 8.2 μM, respectively. This compound is noted for its antidepressant and anxiolytic effects [1] [2].