trpc4

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-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].

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.

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.

N4-benzyl-N2-methylquinazoline-2,4-diamine hydrochloride is an inhibitor of TRPC4.

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

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.

ML204 hydrochloride (ML204 HCl) is a selective and potent TRPC4 TRPC5 channel antagonist that blocks TRPC4β currents activated by intracellular dialysis via μ-opioid receptor stimulation or guanosine 5'-3-O-(thio)trisphosphate (GTPgammaS).

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.

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

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].

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].

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