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) [1][2].

Product Specifications

CAS Number

[72956-44-6]

Product Name Alternative

Desmethylcarvedilol; BM-14242

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Calcium Channel

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling

Field of Research

Metabolic Disease

Purity

97.4

Smiles

OC1=C(OCCNCC(COC2=CC=CC3=C2C4=C(C=CC=C4)N3)O)C=CC=C1

Molecular Formula

C23H24N2O4

Molecular Weight

392.45

Precautions

H302, H315, H319, H335

References & Citations

[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.|[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.