GSK 1702934A

Biological Activity

GSK 1702934A is a potent and selective TRPC3/6 activator (EC₅₀ = 80 and 440 nM for TRPC3 and 6, respectively). Exhibits no activity at TRPV4, TRPA1, M₁, M₄, Ca_V1.2, hERG, Na_V1.5, or CXCR5 receptors at concentrations <10 μmol/L. Induces TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6. Directly activates TRPC channels through by-passing phospholipase-C signaling. Also induces calcium signals in HEK-TRPC6 cells (pEC₅₀ = 6.6).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1.
   Doleschal et al.
   Cardiovasc.Res., 2015;106:163
2. Intensified microwave-assisted N-acylation procedure - Synthesis and activity evaluation of TRPC3 channel agonists with a 1,3-dihydro-2H-benzo[d]imidazol-2-one core.
   Guedes de la Cruz et al.
   Synlett., 2017;28:695
3. Orai and TRPC channel characterization in FceRI-mediated calcium signaling and mediator secretion in human mast cells.
   Wajdner et al.
   Physiol.Rep., 2017;5:e13166

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