GSK 1702934A

Product Description

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).

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Guedes de la Cruz 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. 2017 PMID: 28413263
• Wajdner Orai and TRPC channel characterization in FceRI-mediated calcium signaling and mediator secretion in human mast cells. Physiol.Rep. 2017 PMID: 28292887
• Doleschal TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc.Res. 2015 PMID: 25631581