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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.

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

CAS No.: 3012675-16-7
Formula: C₂₈H₄₆N₂O₃S
Molecular Weight:490.74

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

RyR2 stabilizer-1 Chemical Structure

CAS No.: 3012675-16-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

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]

All Calcium Channel Isoforms :

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.

Chemical Information

CAS No. 3012675-16-7
Molecular Weight 490.74
Formula C₂₈H₄₆N₂O₃S
SMILES

OC1(CCCCN(CCCCN2CC3=C(SCC2)C=CC(OC)=C3)CCCCC4(CC4)O)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Gyuzel Y. Mitronova, et al. 1,4-Benzothiazepines with Cyclopropanol Groups and Their Structural Analogues Exhibit Both RyR2-Stabilizing and SERCA2aStimulating Activities. Journal of Medicinal Chemistry. 2023， Article ASAP. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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