A bradycardic HCN channel blocker
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Zatebradine (hydrochloride)

Item No. 18608

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one, monohydrochloride
CAS Number
91940-87-3
Synonyms
  • UL-FS 49
Molecular Formula
C26H36N2O5 • HCl
Formula Weight
493.0
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
280 nm
SMILES
COC1=CC(CCN(C)CCCN2C(CC(C=C(OC)C(OC)=C3)=C3CC2)=O)=CC=C1OC.Cl
InChi Code
InChI=1S/C26H36N2O5.ClH/c1-27(13-9-19-7-8-22(30-2)23(15-19)31-3)11-6-12-28-14-10-20-16-24(32-4)25(33-5)17-21(20)18-26(28)29;/h7-8,15-17H,6,9-14,18H2,1-5H3;1H
InChi Key
ZRNKXJHEQKMWCH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $117

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    10 mg

    $196

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    25 mg

    $427

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    50 mg

    $796

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    Product Description

    Zatebradine is a bradycardic compound that blocks hyperpolarization-activated inward current (If) through cyclic nucleotide-gated cation (HCN) channels in sinoatrial node cells (IC50s = 1.83, 2.21, 1.9, and 1.88 µM, respectively for HCN1-4 in vitro).1,2 Additionally, it can block voltage-gated outward K+ (IK) currents and related neuronal hyperpolarization-activated inward current (Ih) channels, but exhibits little or no activity for L-type Ca2+ (ICa) currents.3,4 When assessed through telemetric ECG recording in mice, zatebradine reduced heart rate from 600 to 200 beats per minute with an ED50 value of 1.8 mg/kg and induced increasing arrhythmia at concentrations >10 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stieber, J., Wieland, K., Stöckl, G., et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol. Pharmacol. 69(4), 1328-1337 (2006).

    2. Melchiorre, M., Del Lungo, M., Guandalini, L., et al. Design, synthesis, and preliminary biological evaluation of new isoform-selective f-current blockers. J. Med. Chem. 53(18), 6773-6777 (2010).

    3. Satoh, T.O., and Yamada, M. Multiple inhibitory effects of zatebradine (UL-FS 49) on the electrophysiological properties of retinal rod photoreceptors. Pflugers Arch. 443(4), 532-540 (2002).

    4. BoSmith, R.E., Briggs, I., and Sturgess, N.C. Inhibitory actions of ZENECA ZD7288 on whole-cell hyperpolarization activated inward current (If) in guinea-pig dissociated sinoatrial node cells. Br. J. Pharmacol. 110(1), 343-349 (1993).