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.
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- 화학식: C18H14D4N2
- 분자량:266.37
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 53267-01-9
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분자량 266.37
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화학식 C18H14D4N2
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SMILES
[2H]C1([2H])NC(C2CC2(C3=CC=CC=C3)C4=CC=CC=C4)=NC1([2H])[2H]
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Synonyms
Cifenline-d4; Ro 22-7796-d4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[5]. Takahashi Y, et al. Pharmacodynamics of cibenzoline-induced hypoglycemia in rats. Drug Metab Pharmacokinet. 2011 Jun;26(3):242-7. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)