215174-50-8

215174-50-8 structure

Name: Rimacalib
Chemical Name: N'-[3-[(1S)-1-(3-fluoro-4-phenylphenyl)ethyl]-1,2-oxazol-5-yl]morpholine-4-carboximidamide
CAS Number: 215174-50-8
Molecular Formula: C₂₂H₂₃FN₄O₂
Molecular Weight: 394.44200
Catalog: Signaling Pathways Neuronal Signaling CaMK
Create Date: 2017-06-15 23:09:04
Modify Date: 2024-03-01 17:01:29
Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.

Name	N'-[3-[(1S)-1-(3-fluoro-4-phenylphenyl)ethyl]-1,2-oxazol-5-yl]morpholine-4-carboximidamide
Synonyms	Rimacalib SMP 114 4-Morpholinecarboximidamide,N-(3-((1S)-1-(2-fluoro(1,1'-biphenyl)-4-yl)ethyl)-5-isoxazolyl) UNII-BZ76J3N815

Description	Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
Related Catalog	Signaling Pathways >> Neuronal Signaling >> CaMK Research Areas >> Metabolic Disease
Target	CaMKIIα:1 μM (IC50) CaMKIIγ:30 μM (IC50)
In Vitro	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].
Cell Assay	Cardiomyocytes from mice are pre-incubated with Rimacalib (10 μM) for at least 15 min by including the dye in the loading buffer for Ca2+-fluorescent dyes or by pre-incubation in experimental solution for 15 min (patch-clamp experiments)[1].
References	[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.