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Biological Activity for GSK 1702934A
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, CaV1.2, hERG, NaV1.5, 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).
Compound Libraries for GSK 1702934A
Technical Data for GSK 1702934A
|Storage||Store at RT|
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.
Solubility Data for GSK 1702934A
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for GSK 1702934A
The following data is based on the product molecular weight 395.52. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.53 mL||12.64 mL||25.28 mL|
|5 mM||0.51 mL||2.53 mL||5.06 mL|
|10 mM||0.25 mL||1.26 mL||2.53 mL|
|50 mM||0.05 mL||0.25 mL||0.51 mL|
References for GSK 1702934A
References are publications that support the biological activity of the product.
Doleschal et al (2015) TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc.Res. 106 163 PMID: 25631581
Guedes de la Cruz et al (2017) 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. Synlett. 28 695 PMID: 28413263
Wajdner et al (2017) Orai and TRPC channel characterization in FceRI-mediated calcium signaling and mediator secretion in human mast cells. Physiol.Rep. 5 e13166 PMID: 28292887
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Keywords: GSK 1702934A, GSK 1702934A supplier, GSK1702934A, potent, selective, TRPC3, TRPC6, activators, activates, agonists, agonism, TRPC, 6508, Tocris Bioscience
Citations for GSK 1702934A
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Reviews for GSK 1702934A
Average Rating: 4 (Based on 1 Review.)
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I used this product to actvate TRPC channels in HEK293 and Jurkat T cells.