trpc6 in 1

TRPC6-IN-1 is an inhibitor of the Transient Receptor Potential Canonical 6 Channel (TRPC6) (EC50: 4.66 μM).

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.

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.

SAR7334 (TRCP6-IN-1) is a potent and specific inhibitor of TRPC6(IC50 of 7.9 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.

OptoBI-1 is a photochromic, TRPC3/6/7-selective agonist based on a benzimidazole structure, with an EC₅₀ of approximately 0.1 μM for TRPC3 in its active cis conformation. OptoBI-1 can precisely regulate neuronal firing and calcium signaling in endothelial cells, and can be used to study TRPC6-dependent NFAT signaling pathways in mast cells.

TRPC3/6-IN-1 is a highly potent and selective inhibitor that blocks the activity of canonical transient receptor channels TRPC3 and TRPC6, showing significant potency against human isoforms hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. This compound is valuable for research on chronic models of heart failure [1].

TRPC6-IN-3 ((4-(6-Aminopyridazin-3-yl)piperidin-1-yl)(5-(4-fluorophenoxy)-4-methoxypyridin-2-yl)methanone) is an orally active inhibitor of the transient receptor potential canonical 6 (TRPC6) ion channel. It regulates intracellular calcium concentration and influences membrane potential by modulating the flux of cations, including calcium and sodium ions. TRPC6-IN-3 can be used for research on respiratory system-related diseases.

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 ......

Hyp9, a specific agonist for the transient receptor potential canonical 6 (TRPC6) channel, is utilized in spinal cord injury (SCI) research [1].

TRPC3/6-IN-2 is a potent inhibitor of TRPC3 and TRPC6, with IC50 values of 16 nM and 29.8 nM, respectively [1].

Isomaltulose monohydrate is an fMLP inhibitor that also inhibits Src kinase, ERK1/2, p38, and AKT phosphorylation signals in immune regulation. It interferes with the interaction between the βγ subunit of the fMLP receptor Gi protein and downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC₅₀: 1.98 μM), cathepsin G release (IC₅₀: 2.76 μM), and chemotaxis. It can improve excessive activation of neutrophils and reduce inflammation or tissue damage. Derivatives of Isomaltulose monohydrate have been found to inhibit FSGS-related TRPC6 functional mutants [1].