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) [1][2].

Product Specifications

CAS Number

[1794817-24-5]

Product Name Alternative

Desmethylcarvedilol-d5; BM-14242-d5

UNSPSC

12352005

Target

Calcium Channel; Isotope-Labeled Compounds

Related Pathways

Membrane Transporter/Ion Channel; Neuronal Signaling; Others

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease

Smiles

OC(C=CC=C1)=C1OCCNC([2H])([2H])C(O)([2H])C([2H])([2H])OC2=C3C4=CC=CC=C4NC3=CC=C2

Molecular Formula

C23H19D5N2O4

Molecular Weight

397.48

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]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.