Zatebradine hydrochloride

Name: Zatebradine hydrochloride
Brand: Tocris Bioscience
SKU: 2202

Tocris Bioscience, part of Bio-Techne | Catalog # 2202

Citations (5)

COA / SDS

Blocks hyperpolarization-activated current (If)

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Technical Data
Citations

Product Description
Product Specifications
Solubility
Preparing Stock Solutions
Calculators
Background References
Product Documents
Specific Notices

Key Product Details

Description

Blocks hyperpolarization-activated current (If)

Alternative Names

UL-FS 49

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Product Description

Zatebradine hydrochloride is a bradycardic agent that produces use-dependent inhibition of hyperpolarization-activated current I_f (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).

Product Specifications

Molecular Weight

493.04

Formula

C₂₆H₃₆N₂O₅.HCl

Storage

Desiccate at +4°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

Preparing Stock Solutions for Zatebradine hydrochloride

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 all affect the solvent volumes required to prepare stock solutions.

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	0.20 mL	1.01 mL	2.03 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

Calculators

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

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Background References

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

Goethals 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 1993 PMID: 8222132
Romanelli Design, synthesis and preliminary biological evaluation of zatebradine analogues as potential blockers of the hyperpolarization-activated current. Bioorg.Med.Chem. 2005 PMID: 15670930
Van Bogaert Use- and frequency-dependent blockade by UL-FS 49 of the i_f pacemaker current in sheep cardiac Purkinje fibres. Eur.J.Pharmacol. 1990 PMID: 2272362