1. Neuronal Signaling
  2. CaMK
  3. Rimacalib

Rimacalib (Synonyms: SMP 114)

Cat. No.: HY-100779 Purity: 98.75%
Handling Instructions

Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.

For research use only. We do not sell to patients.

Rimacalib Chemical Structure

Rimacalib Chemical Structure

CAS No. : 215174-50-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2750 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3950 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

Rimacalib is a Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.

IC50 & 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].

Clinical Trial
Molecular Weight

394.44

Formula

C₂₂H₂₃FN₄O₂

CAS No.

215174-50-8

SMILES

N=C(N1CCOCC1)NC2=CC([[email protected]](C3=CC=C(C4=CC=CC=C4)C(F)=C3)C)=NO2

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (316.90 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5352 mL 12.6762 mL 25.3524 mL
5 mM 0.5070 mL 2.5352 mL 5.0705 mL
10 mM 0.2535 mL 1.2676 mL 2.5352 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Rimacalib
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