GSK 1702934A

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Description: Potent and selective TRPC3/6 activator
Chemical Name: 1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Citations (1)
Reviews (1)

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

GSK 1702934A is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 1702934A

M. Wt 395.52
Formula C22H25N3O2S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 924377-85-5
PubChem ID 16376051
Smiles O=C(C1=CC2=C(S1)CCCCC2)N3CCC(N4C(NC5=CC=CC=C45)=O)CC3

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
DMSO 39.55 100
ethanol 39.55 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

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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

If you know of a relevant reference for GSK 1702934A, please let us know.

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Keywords: GSK 1702934A, GSK 1702934A supplier, GSK1702934A, potent, selective, TRPC3, TRPC6, activators, activates, agonists, agonism, TRPC, 6508, Tocris Bioscience

1 Citation for GSK 1702934A

Citations are publications that use Tocris products. Selected citations for GSK 1702934A include:

Jonathan H et al (2022) Genetic- and diet-induced ω-3 fatty acid enrichment enhances TRPV4-mediated vasodilation in mice. Cell Rep 40 111306 PMID: 36070688

Do you know of a great paper that uses GSK 1702934A from Tocris? Please let us know.

Reviews for GSK 1702934A

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Activates TRPC channels.
By Sinayat Mahzabeen on 01/29/2021
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HEK 293, Jurkat T cells

I used this product to actvate TRPC channels in HEK293 and Jurkat T cells.