Zatebradine hydrochloride
Based on 2 publication(s) in Google Scholar
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 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.
- Purity: 99.87%
- CAS No.: 91940-87-3
- Formula: C26H37ClN2O5
- Molecular Weight:493.04
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Zatebradine hydrochloride
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Biological Activity
IC50: 1.96 µM (HCN channels)[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57/Bl6-mice [1]
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Dosage:0 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Intraperitoneal injection; for 30 minutes
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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.
Chemical Information
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CAS No. 91940-87-3
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Appearance Solid
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Molecular Weight 493.04
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Formula C26H37ClN2O5
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Color Off-white to light yellow
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SMILES
O=C1N(CCCN(CCC2=CC=C(OC)C(OC)=C2)C)CCC3=CC(OC)=C(OC)C=C3C1.Cl
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Synonyms
UL-FS-49; UL-FS-49CL
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Front Pharmacol
Ivabradine Ameliorates Cardiac Diastolic Dysfunction in Diabetic Mice Independent of Heart Rate Reduction. [Abstract]2021 Jun 22:12:696635. PMID: 34239443 -
Clin Exp Med
SPOP-dependent destabilization of SYT12 in a GSK-3β-dependent manner in papillary thyroid cancer cells. [Abstract]2025 Jul 10;25(1):243. PMID: 40640517
Solvent & Solubility
H2O : 100 mg/mL (202.82 mM; Need ultrasonic)
DMSO : 100 mg/mL (202.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 110 mg/mL (223.11 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Stieber J, et al. Bradycardic and proarrhythmic properties of sinus node inhibitors. Mol Pharmacol. 2006 Apr;69(4):1328-37. Epub 2005 Dec 30. [Content Brief]
[2]. Van Bogaert PP, et al. Use-dependent blockade of cardiac pacemaker current (If) by cilobradine and zatebradine. Eur J Pharmacol. 2003 Oct 8;478(2-3):161-71. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.0282 mL | 10.1412 mL | 20.2823 mL | 50.7058 mL |
| 5 mM | 0.4056 mL | 2.0282 mL | 4.0565 mL | 10.1412 mL | |
| 10 mM | 0.2028 mL | 1.0141 mL | 2.0282 mL | 5.0706 mL | |
| 15 mM | 0.1352 mL | 0.6761 mL | 1.3522 mL | 3.3804 mL | |
| 20 mM | 0.1014 mL | 0.5071 mL | 1.0141 mL | 2.5353 mL | |
| 25 mM | 0.0811 mL | 0.4056 mL | 0.8113 mL | 2.0282 mL | |
| 30 mM | 0.0676 mL | 0.3380 mL | 0.6761 mL | 1.6902 mL | |
| 40 mM | 0.0507 mL | 0.2535 mL | 0.5071 mL | 1.2676 mL | |
| 50 mM | 0.0406 mL | 0.2028 mL | 0.4056 mL | 1.0141 mL | |
| 60 mM | 0.0338 mL | 0.1690 mL | 0.3380 mL | 0.8451 mL | |
| 80 mM | 0.0254 mL | 0.1268 mL | 0.2535 mL | 0.6338 mL | |
| 100 mM | 0.0203 mL | 0.1014 mL | 0.2028 mL | 0.5071 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Zatebradine hydrochloride Related Classifications
HY-13422 Related Classifications
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