Fig. 1 · Structure
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O-Desmethylcarvedilol
RyR2R4496C Inhibitor
O-Desmethylcarvedilol is an inhibitor of the ryanodine receptor 2 (RyR2) R4496C mutation. This active metabolite of Carvedilol effectively reduces store-overload-induced calcium release in HEK293 cells with the RyR2 R4496C mutation, exhibiting an IC50 of 7.62 µM. Additionally, O-Desmethylcarvedilol mitigates the increases in heart rate and decreases in diastolic blood pressure induced by Isoproterenol in conscious rabbits, with ED50 values of 32 and 5 µg/kg, respectively. Its unique biological activity makes it a valuable tool for research into calcium signaling and cardiovascular responses.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Inhibitor |
| CAS Number | 72956-44-6 |
| Applications | RyR2R4496C Inhibitor |
| Formula | C23H24N2O4 |
| Molecular Weight | 392.45 |
| Synonyms | Desmethylcarvedilol; BM-14242 |
| SMILES | OC1=C(OCCNCC(COC2=CC=CC3=C2C4=C(C=CC=C4)N3)O)C=CC=C1 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.