GSK 1702934A

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Cat.No. 6508 - GSK 1702934A | C22H25N3O2S | CAS No. 924377-85-5
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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).

Technical Data

M. Wt 395.52
Formula C22H25N3O2S
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 924377-85-5
PubChem ID 16376051
InChI Key AXWRAIIIBRLXBP-UHFFFAOYSA-N
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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.55 100
ethanol 39.55 100

Preparing Stock Solutions

The following data is based on the product molecular weight 395.52. Batch specific molecular weights may vary from batch to batch due to solvent 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

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References

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

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