RyR2 stabilizer-1
RyR2 stabilizer-1 (compound 12a) is a potent RyR2 stabilizer and SERCA2a activator with EC50s of 2.7 μM for RyR2 and 383 nM for SERCA2. RyR2 stabilizer-1 inhibits Ca2+ leakage from the SR RyR2 while promoting SERCA2 to pump Ca2+ back to SR, which make RyR2 stabilizer-1 possible to prevent cardiac arrhythmias.
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- CAS No.: 3012675-16-7
- Formule: C28H46N2O3S
- Masse moléculaire:490.74
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
Ryanodine receptor type 2 (RyR2) EC50: 2.7 μM (HEK-293)[1]; sarco/endoplasmic reticulum Ca2+-ATPase 2a (SERCA2a) EC50: 383 nM(mouse SR)[1]
In Vitro
RyR2 stabilizer-1 (0-100 μM) significantly increases [Ca2+]ER dose-dependently, at concentrations above 25 μM RyR2 stabilizer-1 demonstrates the most pronounced effect[1].
RyR2 stabilizer-1 has EC50s of 383 nM, 9.2 μM and 16 nM for SERCA2a in mouse SR, HL-1 and HEK ER, respectively[1].
RyR2 stabilizer-1 (10 μM, incubated for 2 h) improves HL-1 SERCA2a activity in the caffeine-induced Ca2+ release assay[1].
RyR2 stabilizer-1 (50 μM, HL-1, 24h) shows no significant cell death in CytoTox-Glo Cytotoxicity Assay[1].
RyR2 stabilizer-1 (100 μM, 5min) causes a strong decrease in NADH fluorescence which reflecting an increase in SERCA2a activity in SR microsomes derived from mouse heart ventricles, it also causes the improvement of ATPase activity [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 3012675-16-7
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Masse moléculaire 490.74
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Formule C28H46N2O3S
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SMILES
OC1(CCCCN(CCCCN2CC3=C(SCC2)C=CC(OC)=C3)CCCCC4(CC4)O)CC1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RyR2 stabilizer-1 Related Classifications
HY-149779 Related Classifications
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