GSK1702934A is a selective TRPC3 agonist. GSK1702934A modulates cardiac contractility and f arrhythmogenesis by activation of TRPC3.
性状
Solid
IC50 & Target[1][2]
TRPC3
体外研究(In Vitro)
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.GSK1702934A induces a transient, non-selective conductance and prolonged action potentials in TRPC3-overexpressing myocytes but not in wild-type myocytes.GSK1702934A substantially promotes NCX currents in TRPC3-overexpressing myocytes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GSK1702934A (0.3-3 mg/kg; i.v.) transiently increases blood pressure by 15 ~ 35 mmHg in conscious Sprague Dawley rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[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.
溶解度数据
In Vitro: DMSO : 100 mg/mL (252.83 mM; Need ultrasonic)配制储备液