GSK1702934A

• CAT Number: I006897
• CAS Number: 924377-85-5
• Molecular Formula: C22H25N3O2S
• Molecular Weight: 395.52
• Purity: ≥95%
• Synonyms: 3-[1-(5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one
• InChI: InChI=1S/C22H25N3O2S/c26-21(20-14-15-6-2-1-3-9-19(15)28-20)24-12-10-16(11-13-24)25-18-8-5-4-7-17(18)23-22(25)27/h4-5,7-8,14,16H,1-3,6,9-13H2,(H,23,27)
• InChIKey: AXWRAIIIBRLXBP-UHFFFAOYSA-N
• SMILES: C1CCC2=C(CC1)SC(=C2)C(=O)N3CCC(CC3)N4C5=CC=CC=C5NC4=O

GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3[1][2].
GSK1702934A is able to induce TRPC3/6-currents in HEK293 cells transduced with recombinant human TRPC3/6 with an EC50 of 0.08 mM and 0.44 mM, respectively[1].
GSK1702934A induces a transient, non-selective conductance and prolonged action potentials in TRPC3-overexpressing myocytes but not in wild-type myocytes[2].
GSK1702934A substantially promotes NCX currents in TRPC3-overexpressing myocytes[2].
GSK1702934A (0.3-3 mg/kg; i.v.) transiently increases blood pressure by 15 ~ 35 mmHg in conscious Sprague Dawley rats[3].

Reference

[1]. de la Cruz GG, et al. 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 Apr;28(6):695-700.
 [Content Brief]

[2]. Doleschal B, et al. TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1. Cardiovasc Res. 2015 Apr 1;106(1):163-73.
 [Content Brief]

[3]. Xu, X., et al. Schnackenberg, C. G. Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists. Biophysical Journal, 2013. 104(2), 454a.