Cilobradine (hydrochloride)
Product Specifications
UNSPSC Description
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.
Target: HCN Channel blocker
Cilobradine 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).
Target Antigen
HCN Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Applications
Neuroscience-Neuromodulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/Cilobradine-hydrochloride.html
Purity
99.0
Solubility
DMSO : ≥ 125 mg/mL|H2O : 100 mg/mL (ultrasonic)
Smiles
O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl
Molecular Weight
519.07
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-18940A/Cilobradine-hydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-18940A/Cilobradine-hydrochloride-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
186097-54-1
Available Sizes
Curated Selection
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