Bioactivity | Rimacalib (SMP 114) is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ[1]. | |||||||||
Invitro | Rimacalib (SMP-114) improves (by ~40%) Ca2+-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)[1]. | |||||||||
Name | Rimacalib | |||||||||
CAS | 215174-50-8 | |||||||||
Formula | C22H23FN4O2 | |||||||||
Molar Mass | 394.44 | |||||||||
Appearance | Solid | |||||||||
Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
Storage |
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Reference | [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. |