2. Membrane Transporter/Ion Channel
  3. HCN Channel
  4. Zatebradine

Zatebradine  (Synonyms: UL-FS-49 free base; UL-FS-49CL free base)

Cat. No.: HY-13422A Purity: 99.59%
COA Handling Instructions

Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current 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.

For research use only. We do not sell to patients.

Zatebradine Chemical Structure

Zatebradine Chemical Structure

CAS No. : 85175-67-3

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Solution
10 mM * 1 mL in DMSO USD 94 In-stock
Oil + Solvent
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10 mg USD 135 In-stock
50 mg USD 588 In-stock
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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Zatebradine

  • Biological Activity

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  • References

  • Customer Review

Description

Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current 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[1].

IC50 & Target

IC50: 1.96 µM (HCN channels)[1]
In Vitro

The use-dependent blockade by Zatebradine of the cardiac pacemaker current from rabbit sino-atrial node cells has an apparent Kd of 480 nM[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

Zatebradine (0-20 mg/kg; intraperitoneal injection; for 30 minutes; male C57/Bl6-mice) reduces the heart rate dose-dependently from 600 to 200 bpm with ED50 value of 1.8 mg/kg and induces increasing arrhythmia[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male C57/Bl6-mice [1]
Dosage: 0 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg
Administration: Intraperitoneal injection; for 30 minutes
Result: Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight.
Molecular Weight

456.57

Appearance

Oil

Formula

C26H36N2O5
CAS No.
SMILES

O=C1N(CCCN(CCC2=CC=C(OC)C(OC)=C2)C)CCC3=CC(OC)=C(OC)C=C3C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

Ethanol : 100 mg/mL (219.02 mM; Need ultrasonic)

DMSO : ≥ 50 mg/mL (109.51 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1902 mL 10.9512 mL 21.9024 mL
5 mM 0.4380 mL 2.1902 mL 4.3805 mL
10 mM 0.2190 mL 1.0951 mL 2.1902 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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Keywords:

Zatebradine85175-67-3UL-FS-49UL-FS-49CLHCN ChannelHyperpolarization activated cyclic nucleotide gated channelsInhibitorinhibitorinhibit

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