Cilobradine hydrochloride
Zilobradine hydrochloride (CAS No.: 186097-54-1) is a hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker, with a half-maximal inhibitory concentration (IC₅₀) of 0.62 micromolar (μM) in mouse sinoatrial node cells [1].
Zilobradine hydrochloride can slow the heart rate by reducing the spontaneous firing frequency of the cardiac sinoatrial node [2]. In mouse experiments, telemetry electrocardiogram (ECG) recordings showed that this drug reduces heart rate in a dose-dependent manner, with a half-maximal effective dose (ED₅₀) of 1.2 milligrams per kilogram (mg/kg). In addition, at concentrations above 5 mg/kg, zilobradine hydrochloride also exhibits proarrhythmic effects [1].
Reference:
[1] Stieber J, Wieland K, Stöckl G, Ludwig A, Hofmann F. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006 Apr;69(4):1328-37. doi: 10.1124/mol.105.020701. Epub 2005 Dec 30. PMID: 16387796.
[2] Bois, P., Chatelier, A., Bescond, J., Faivre, JF. (2011). Pharmacology of Hyperpolarization-Activated Cyclic Nucleotide-Gated (HCN) Channels. In: Gupta, S. (eds) Ion Channels and Their Inhibitors. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-19922-6_2
| Storage | Store at -20°C |
| M.Wt | 519.08 |
| Cas No. | 186097-54-1 |
| Formula | C28H38N2O5·HCl |
| Synonyms | DK-AH 269 |
| Solubility | Soluble in DMSO |
| Chemical Name | (S)-3-((1-(3,4-dimethoxyphenethyl)piperidin-3-yl)methyl)-7,8-dimethoxy-1,3,4,5-tetrahydro-2H-benzo[d]azepin-2-one hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | COC1=C(OC)C=C(CCN(C[C@H]2CCCN(CCC3=CC=C(OC)C(OC)=C3)C2)C(C4)=O)C4=C1.Cl |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
