General description

A cell permeable hydroxytricyclic derivative that acts as a specific and reversible inhibitor of transient receptor potential melastatin 4 (TRPM4) (IC₅₀ = 20 µM in HEK293 cells). Does not affect TRPM5 and cystic fibrosis transmembrane conductance regulators (CFTR) channels. Decreases the occurrence of early after depolarizations (EAD) and exhibits an anti-arrhythmic effect that is independent of the action of protein kinase A. Shown to abolish NMDA-induced burst firing in dopaminergic neurons. Does not affect K+ currents at ~10 µM, but at higher concentration (~100 µM) it reversibly reduces K+ currents.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Grand, T., et al. 2008. Brit. Journ. Pharm.153, 1697.Simard, C., 2012. Brit. Journ. Pharm.165, 2354.

Packaging

Packaged under inert gas

50 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Irritant (B)