2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. 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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RyR2 stabilizer-1 Chemical Structure

RyR2 stabilizer-1 Chemical Structure

CAS No. : 3012675-16-7

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RyR2 stabilizer-1 Related Antibodies

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Description

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[1].

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.

RyR2 stabilizer-1 Related Antibodies
Molecular Weight

490.74

Formula

C28H46N2O3S
CAS No.
SMILES

OC1(CCCCN(CCCCN2CC3=C(SCC2)C=CC(OC)=C3)CCCCC4(CC4)O)CC1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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RyR2 stabilizer-1 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RyR2 stabilizer-13012675-16-7Calcium ChannelCa2+ channelsCa channelsCardiovascular DiseaseRyR2SERCA2aHEK-293THL-1Cardiac ArrhythmiasC57BL/6N miceInhibitorinhibitorinhibit

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