Rimacalib (SMP 114) is a Ca/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC 50 s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
性状
Solid
IC50 & Target[1][2]
CaMK IIα 1 μM (IC50) CaMK IIγ 30 μM (IC
体外研究(In Vitro)
Rimacalib (SMP-114) improves (by ~40%) Ca-transient potentiation during the 30 s stimulation pause, higher Fura-2 transient amplitude after the pause upon Rimacalib vs. 37.2±4.3% in control, n=60/17 cells/mice vs. n=65/17, p<0.05) and in parallel cardiomyocyte contractility (135.0±15.4% vs. 97.2±16% increase of twitch amplitude, p=0.098). 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
ClinicalTrial
参考文献
[1]. Neef S, et al. Reduction of SR Ca2+ leak and arrhythmogenic cellular correlates by SMP-114, a novel CaMKII inhibitor with oral bioavailability. Basic Res Cardiol. 2017 Jul;112(4):45.
溶解度数据
In Vitro: DMSO : 125 mg/mL (316.90 mM; Need ultrasonic)配制储备液