TRPC3 6-IN-1 is a highly potent and selective inhibitor that specifically blocks the activity of the canonical transient receptor channels TRPC3 and TRPC6. It exhibits a significant blocking potency against the human isoforms hTRPC3 and hTRPC6, with IC50 values of 1260 nM and 500 nM, respectively. This compound, TRPC3 6-IN-1, is particularly valuable for conducting research on chronic models of heart failure [1].
GSK 2833503A is a potent and selective TRPC6 and TRPC3 antagonist (IC50 = 3-16 nM and 21-100 nM, respectively). GSK 2833503A exhibits >63-fold selectivity over other ion channels, including other TRP channels, CaV1.2, hERG and NaV1.5. GSK 2833503A suppresses angiotensin II or endothelin-1-induced cardiac hypertrophy signaling in HEK293 cellsin vitroand in cardiomyocytes.
Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg/kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......
GSK2332255B is a highly potent and selective TRPC3 and TRPC6 antagonist, exhibiting IC50 values of 5 nM and 4 nM for rat TRPC3 and rat TRPC6, respectively. Furthermore, GSK2332255B demonstrates exceptional selectivity, surpassing a ≥100-fold difference when compared to other calcium-permeable channels.
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