For research use only. Not for therapeutic Use.
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].
| Catalog Number | I006897 |
| CAS Number | 924377-85-5 |
| Synonyms | 3-[1-(5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-2-carbonyl)piperidin-4-yl]-1H-benzimidazol-2-one |
| Molecular Formula | C22H25N3O2S |
| Purity | ≥95% |
| 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 |
| 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. [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. [3]. Xu, X., et al. Schnackenberg, C. G. Characterization of Small Molecule TRPC3 and TRPC6 agonist and Antagonists. Biophysical Journal, 2013. 104(2), 454a. |
