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MedChemExpress - Model Cibenzoline -53267-01-9
MCE products for research use only. We do not sell to patients.
Cibenzoline
MCE China：Cibenzoline
Brand：MedChemExpress (MCE)
Cat. No.HY-106577
CAS：53267-01-9
Synonyms：Cifenline; Ro 22-7796
Purity：99.96%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：Cibenzoline (1-100 μM; 3-5 min) inhibits the spontaneous activity and leads to sinus arrest in rat sino-atrial nodal cells[1]. Cibenzoline (3-300 μM; 15 minutes) inhibits IKr and IKs currents with IC50 values of 8.8 μM and 12.3 μM in rat sino-atrial nodal cells[1].
In Vivo：Cibenzoline (5-20 mg/kg; intravenous injection; single dose) has hypoglycemic effect in rats[2]. Pharmacokinetic Analysis in Rats[2] Route Dose (mg/kg) k12 (h-1) k21 (h-1) Vc (L/kg) Vmax, CBZ (μg/h) Km, CBZ (μg/L) i.v. 5, 10 and 20 1.93 1.01 4.70 32391 3554
IC50 & Target：KATP channel[1] Cellular Effect Cell Line Type Value Description References
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References：
[1]. 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]
[2]. Takahashi Y, et al. Pharmacodynamics of cibenzoline-induced hypoglycemia in rats. Drug Metab Pharmacokinet. 2011 Jun;26(3):242-7. [Content Brief]
[3]. 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]
[4]. 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]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。