Cilobradine [CAS 147541-45-5]

Cilobradine (Cilo) is a HCN channel blocker with heart rate reducing activity. Cilobradine blocks the slow inward current of human HCN1, HCN2, HCN3, and HCN4 channels. Cilobradine has a slightly higher efficiency in blocking endogenous If in mouse sinoatrial node cells (IC50 value is 0.62μM) . Cilobradine can dose-dependently reduce the heart rate from 600 to 200 bpm with an ED50 value of 1.2 mg/kg. Cilobradine induces arrhythmias at doses greater than 5 mg/kg, which are characterized by periodic fluctuations between T waves and P waves[1].

[147541-45-5]

C28H38N2O5

482.61

O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1

Endogenous Metabolite

Room temperature