Cilobradine hydrochloride

• CAT Number: I002399
• CAS Number: 186097-54-1
• Molecular Formula: C28H38N2O5 • HCl
• Molecular Weight: 519.1
• Purity: ≥95%
• Synonyms: Cilobradine
• Target: HCN Channel
• Solubility: 10 mM in H2O
• Storage: -20°C
• InChIKey: MTAKUIYCCYKGJJ-UHFFFAOYSA-N

Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.Target: HCN Channel blockerCilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).

Reference

[1]. Cheng L, et al. Molecular mapping of the binding site for a blocker of hyperpolarization-activated, cyclic nucleotide-modulated pacemaker channels. J Pharmacol Exp Ther. 2007 Sep;322(3):931-939.