An HCN channel blocker
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DK-AH 269

Item No. 21425

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[(3S)-1-[2-(3,4-dimethoxyphenyl)ethyl]-3-piperidinyl]methyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one, monohydrochloride
CAS Number
186097-54-1
Synonyms
  • Cilobradine
Molecular Formula
C28H38N2O5 • HCl
Formula Weight
519.1
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 3 mg/mlEthanol: 0.5 mg/mlPBS (pH 7.2): 2 mg/ml
λmax
281 nm
SMILES
COC1=CC=C(CCN2CC(CN(CCC(C=C(OC)C(OC)=C3)=C3C4)C4=O)CCC2)C=C1OC.Cl
InChi Code
InChI=1S/C28H38N2O5.ClH/c1-32-24-8-7-20(14-25(24)33-2)9-12-29-11-5-6-21(18-29)19-30-13-10-22-15-26(34-3)27(35-4)16-23(22)17-28(30)31;/h7-8,14-16,21H,5-6,9-13,17-19H2,1-4H3;1H
InChi Key
MTAKUIYCCYKGJJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $185

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    10 mg

    $347

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    25 mg

    $811

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    Product Description

    DK-AH 269 blocks hyperpolarization-activated cyclic nucleotide-gated (HCN) channels (IC50 = 0.62 µM in mouse sinoatrial node cells).1 DK-AH 269 slows heart rate by decreasing the spontaneous firing rate of the sinoatrial node in the heart.2 Using telemetric ECG recordings in mice, it reduced heart rate in a dose-dependent fashion with an ED50 of 1.2 mg/kg.1 DK-AH 269 also has proarrhythmic properties at concentrations higher than 5 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. Bois, P., Chatelier, A., Bescond, J., et al. Pharmacology of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels. Ion channels and their inhibitors 33-51 (2011).