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GSK1702934A | TRPC 3/6 activator

GSK1702934A is a TRPC3 activator.  In whole-cell patch-clamp experiments in HEK293 cells transduced with recombinant human TRPC3 or TRPC6, GSK-1702934A activated the TRPC3 and TRPC6 current with EC50 of 0.08 mM and 0.44 mM respectively. In the rat cardiomyocyte-like cell line H9C2 GSK-1702934A  (1mM) activated TRPC6-like current  and was completely blocked by GSK-417651A. It transiently increased the perfusion pressure of isolated rat heart retrogradely perfused via aortic cannulation at 1mM.1 Induces pro-arrhythmic and inotropic effects in TRPC3-overexpressing monocytes.2

References/Citations

1) Xu et al. (2013) Characterization of Small Molecule TRPC3 and TRPC6 Agonists and Antagonists; Proceedings of the Biophysical Soc., 104(2) 454a
2) Doleschal et al. (2015) TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1.; Cardiovasc. Res., 106 163

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Focus Biomolecules cell signaling reagent supplier, chemical structure of GSK1702934A | TRPC 3/6 activator | CAS 924377-85-5

Catalog#  10-1445

$110.00
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Catalog Number:
10-1445
CAS:
924377-85-5
Activity:
TRPC3/6 activator
Chemical Name:
1-(1-(5,6,7,8-Tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl)-1H-benzo[d]- imidazole-2(3H)-one
Molecular Weight:
396.53
Molecular Formula:
C22H26N3O2S
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml with warming)
Physical Properties:
White solid
Purity:
98% by TLC
Storage Temperature:
Room temperature (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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