| Identification | Back Directory | [Name]
1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one | [CAS]
924377-85-5 | [Synonyms]
GSK 1702934A
1,3-Dihydro-1-[1-[(5,6,7,8-tetrahydro-4H-cyclohepta[b]thien-2-yl)carbonyl]-4-piperidinyl]-2H-benzimidazol-2-one | [Molecular Formula]
C22H25N3O2S | [MDL Number]
MFCD08868156 | [MOL File]
924377-85-5.mol | [Molecular Weight]
395.52 |
| Chemical Properties | Back Directory | [storage temp. ]
RT | [solubility ]
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 25 mg/ml with warming) | [form ]
solid | [color ]
White | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. |
| Hazard Information | Back Directory | [Description]
GSK1702934A (924377-85-5) is a TRPC3 activator.? In whole-cell patch-clamp experiments in HEK293 cells transduced with recombinant human TRPC3 or TRPC6, GSK-1702934A activated the TRPC3 and TRPC6 current with EC50?of 0.08?mM and 0.44?mM respectively. In the rat cardiomyocyte-like cell line H9C2 GSK-1702934A? (1mM) activated TRPC6-like current? and was completely blocked by GSK-417651A. It transiently increased the perfusion pressure of isolated rat heart retrogradely perfused via aortic cannulation at 1mM.1?Induces pro-arrhythmic and inotropic effects in TRPC3-overexpressing monocytes.2 | [Uses]
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). | [storage]
Store at RT | [References]
1) Xu?et al. (2013)?Characterization of Small Molecule TRPC3 and TRPC6 Agonists and Antagonists; Proceedings of the Biophysical Soc.,?104(2)?454a
2)?Doleschal?et al.?(2015)?TRPC3 contributes to regulation of cardiac contractility and arrhythmogenesis by dynamic interaction with NCX1.; Cardiovasc. Res.,?106?163 |
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BOC Sciences
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16314854226 |
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www.bocsci.com |
| Company Name: |
MedChemExpress
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021-58955995 |
| Website: |
www.medchemexpress.com |
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