Cibenzoline-d4

Cibenzoline-d4 (Cifenline-d4) is deuterium labeled Cibenzoline. Cibenzoline is a class Ia antiarrhythmic active molecule with low anticholinergic activity. Cibenzoline is a KATP channel inhibitor, acting through the pore forming subunit Kir6.2, with an IC50 of 22.2 μM. Cibenzoline inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM, respectively. Cibenzoline is used in the study of cardiac diseases. In addition, Cibenzoline can induce hypoglycemia[1][2][3][4].

Product Specifications

Product Name Alternative

Cifenline-d4; Ro 22-7796-d4

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Potassium Channel

Related Pathways

Membrane Transporter/Ion Channel; Others

Applications

Metabolism-protein/nucleotide metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease

Smiles

[2H]C1([2H])NC(C2CC2(C3=CC=CC=C3)C4=CC=CC=C4)=NC1([2H])[2H]

Molecular Formula

C18H14D4N2

Molecular Weight

266.37

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Mukai E, et al. The antiarrhythmic agent cibenzoline inhibits KATP channels by binding to Kir6.2. Biochem Biophys Res Commun. 1998;251 (2) :477-481.|[3]Hamada M, et al. Class Ia antiarrhythmic drug cibenzoline: a new approach to the medical treatment of hypertrophic obstructive cardiomyopathy. Circulation. 1997;96 (5) :1520-1524.|[4]Satoh H. Comparative actions of cibenzoline and disopyramide on I (Kr) and I (Ks) currents in rat sino-atrial nodal cells. Eur J Pharmacol. 2000 Oct 27;407 (1-2) :123-9.|[5]Takahashi Y, et al. Pharmacodynamics of cibenzoline-induced hypoglycemia in rats. Drug Metab Pharmacokinet. 2011 Jun;26 (3) :242-7.