Rimacalib

Names

[ Name ]:
Rimacalib

[Synonym ]:
Rimacalib
SMP 114
4-Morpholinecarboximidamide,N-(3-((1S)-1-(2-fluoro(1,1'-biphenyl)-4-yl)ethyl)-5-isoxazolyl)
UNII-BZ76J3N815

Biological Activity

[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.

[Related Small Molecules]

KN-93 | STO609 | KN-62 | KN-92-hydrochloride | CaMKII-IN-1 | MLCK inhibitor peptide 18 | Autocamtide-2 | A 484954 | Calmodulin-Dependent Protein Kinase II (290-309) | Metofenazate | NH 125 | Syntide 2 trifluoroacetate salt

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₃FN₄O₂

[ Molecular Weight ]:
394.44200

[ Exact Mass ]:
394.18100

[ PSA ]:
74.38000

[ LogP ]:
4.42200

[ Storage condition ]:
2-8℃