72956-44-6
Chemical Structure
O-Desmethylcarvedilol
Synonym(s): Desmethylcarvedilol; BM-14242
- CAS No.: 72956-44-6
- Formula:C23H24N2O4
- Molecular Weight:392.45
IUPAC Name: 2-(2-((3-((9H-carbazol-4-yl)oxy)-2-hydroxypropyl)amino)ethoxy)phenol
InChIKey: XAUKPPPYYOKVQJ-UHFFFAOYSA-N
SMILES: OC1=C(OCCNCC(COC2=CC=CC3=C2C4=C(C=CC=C4)N3)O)C=CC=C1
Biological Activity: O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively)[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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O-Desmethylcarvedilol | 97.4% | O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 µM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED50s = 32 and 5 µg/kg, respectively). | ||||||||||||||||||||
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O-Desmethyl carvedilol-d5 | O-Desmethyl carvedilol-d5 (Desmethylcarvedilol-d5) is deuterium labeled O-Desmethylcarvedilol. O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of the non-selective β-adrenergic receptor (β-AR) antagonist Carvedilol (HY-B0006). O-Desmethylcarvedilol inhibits store-overload-induced calcium release in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 7.62 μM). O-Desmethylcarvedilol reduces increases in heart rate and prevents decreases in diastolic blood pressure induced by Isoproterenol (HY-B0468) in conscious rabbits (ED50s = 32 and 5 μg/kg, respectively). | |||||||||||||||||||||
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References
- [1]. Chris D Smith, et al. Novel carvedilol analogues that suppress store-overload-induced Ca2+ release. J Med Chem. 2013 Nov 14;56(21):8626-55. [Content Brief]
- [2]. K Strein, et al. Pharmacological profile of carvedilol, a compound with β-blocking and vasodilating properties. J Cardiovasc Pharmacol. 1987:10 Suppl 11:S33-41. [Content Brief]
