Zatebradine hydrochloride

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Cat.No. 2202 - Zatebradine hydrochloride | C26H36N2O5.HCl | CAS No. 91940-87-3
Description: Blocks hyperpolarization-activated current (If)
Alternative Names: UL-FS 49
Chemical Name: 3-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (5)

Biological Activity

Bradycardic agent that produces use-dependent inhibition of hyperpolarization-activated current If (HCN channel) in sinoatrial node cells (EC50 = 480 nM) and Purkinje fibres. Displays negative chronotropic activity in isolated guinea pig atria (EC50 of 13.4 μM).

Technical Data

M. Wt 493.04
Formula C26H36N2O5.HCl
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 91940-87-3
PubChem ID 3045335
InChI Key ZRNKXJHEQKMWCH-UHFFFAOYSA-N
Smiles Cl.COC1=CC=C(CCN(C)CCCN2CCC3=C(CC2=O)C=C(OC)C(OC)=C3)C=C1OC

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 49.3 100

Preparing Stock Solutions

The following data is based on the product molecular weight 493.04. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.03 mL 10.14 mL 20.28 mL
5 mM 0.41 mL 2.03 mL 4.06 mL
10 mM 0.2 mL 1.01 mL 2.03 mL
50 mM 0.04 mL 0.2 mL 0.41 mL

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References

References are publications that support the biological activity of the product.

Van Bogaert et al (1990) Use- and frequency-dependent blockade by UL-FS 49 of the if pacemaker current in sheep cardiac Purkinje fibres. Eur.J.Pharmacol. 187 241 PMID: 2272362

Goethals et al (1993) Use-dependent block of the pacemaker current I(f) in rabbit sinoatrial node cells by zatebradine (UL-FS 49). On the mode of action of sinus node inhibitors. Circulation 88 2389 PMID: 8222132

Romanelli et al (2005) Design, synthesis and preliminary biological evaluation of zatebradine analogues as potential blockers of the hyperpolarization-activated current. Bioorg.Med.Chem. 13 1211 PMID: 15670930


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1 Citation for Zatebradine hydrochloride

Citations are publications that use Tocris products. Selected citations for Zatebradine hydrochloride include:

Bender et al (2007) Localization of HCN1 channels to presynaptic compartments: novel plasticity that may contribute to hippocampal maturation. J Neurosci 27 4697 PMID: 17460082


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Literature in this Area

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