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Zatebradine hydrochloride

Catalog No. T13387L CAS 91940-87-3

Synonyms: UL-FS-49, UL-FS-49CL

Zatebradine hydrochloride is a highly effective and effective HCN Channel inhibitor (IC50:1.96 µM). HCN Channel is an effective hyperpolarization activated loop nucleotide gated channel. Zatebradine hydrochloride blocks slow inward currents through human HCN1, HCN2, HCN3, and HCN4 channels with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM, and 1.88 µM, respectively.

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Zatebradine hydrochloride, CAS 91940-87-3

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Zatebradine hydrochloride is a highly effective and effective HCN Channel inhibitor (IC50:1.96 µM). HCN Channel is an effective hyperpolarization activated loop nucleotide gated channel. Zatebradine hydrochloride blocks slow inward currents through human HCN1, HCN2, HCN3, and HCN4 channels with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM, and 1.88 µM, respectively.
Targets&IC50	HCN channels:1.96 μM, HCN1:1.83 µm, HCN2:2.21 µM, HCN3:1.90 µM, HCN4:1.88 µM
In vitro	Zatebradine demonstrates a use-dependent inhibitory effect on the cardiac pacemaker current in rabbit sino-atrial node cells, with an observed Kd value of 480 nM.[2]
In vivo	Zatebradine hydrochloride (0-20 mg/kg; i.p.; for 30 minutes; male C57/Bl6-mice) decreases the heart rate dose-dependently from 600 to 200 bpm (ED50: 1.8 mg/kg).[1]

Synonyms	UL-FS-49, UL-FS-49CL
Molecular Weight	493.04
Formula	C26H37ClN2O5
CAS No.	91940-87-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 90.0 mg/mL (182.5 mM), Need ultrasonic

H2O: 90.0 mg/mL (182.5 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Stieber J, et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006;69(4):1328-37. 2. Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003;478(2-3):161-71.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zatebradine hydrochloride 91940-87-3 Membrane transporter/Ion channel Others HCN Channel UL-FS-49 UL-FS-49CL Inhibitor inhibitor inhibit

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