Chubanov, V.; Schnitzler, M. Mederos; Meissner, M.; Schaefer, S.; Abstiens, K.; Hofmann, T.; Gudermann, T. published an article in British Journal of Pharmacology. The title of the article was 《Natural and synthetic modulators of SK (KCa2) potassium channels inhibit magnesium-dependent activity of the kinase-coupled cation channel TRPM7》.HPLC of Formula: 70006-24-5 The author mentioned the following in the article:
Background and Purpose Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a bifunctional protein comprising a TRP ion channel segment linked to an α-type protein kinase domain. TRPM7 is essential for proliferation and cell growth. Up-regulation of TRPM7 function is involved in anoxic neuronal death, cardiac fibrosis and tumor cell proliferation. The goal of this work was to identify non-toxic inhibitors of the TRPM7 channel and to assess the effect of blocking endogenous TRPM7 currents on the phenotype of living cells. Exptl. Approach We developed an aequorin bioluminescence-based assay of TRPM7 channel activity and performed a hypothesis-driven screen for inhibitors of the channel. The candidates identified were further assessed electrophysiol. and in cell biol. experiments Key Results TRPM7 currents were inhibited by modulators of small conductance Ca2+-activated K+ channels (KCa2.1-2.3; SK) channels, including the antimalarial plant alkaloid quinine, CyPPA, dequalinium, NS8593, SKA31 and UCL 1684. The most potent compound NS8593 (IC50 1.6 μM) specifically targeted TRPM7 as compared with other TRP channels, interfered with Mg2+-dependent regulation of TRPM7 channel and inhibited the motility of cultured cells. NS8593 exhibited full and reversible block of native TRPM7-like currents in HEK 293 cells, freshly isolated smooth muscle cells, primary podocytes and ventricular myocytes. Conclusions and Implications This study reveals a tight overlap in the pharmacol. profiles of TRPM7 and KCa2.1-2.3 channels. NS8593 acts as a neg. gating modulator of TRPM7 and is well-suited to study functional features and cellular roles of endogenous TRPM7. In the part of experimental materials, we found many familiar compounds, such as Abt-724(cas: 70006-24-5HPLC of Formula: 70006-24-5)
Abt-724(cas: 70006-24-5) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).HPLC of Formula: 70006-24-5
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics