[CAS NO. 91940-87-3] Zatebradinehydrochloride
PRODUCTS SPECIFICATIONS [91940-87-3]
DESCRIPTION [91940-87-3]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 493.04 |
| Molecular Formula | C26H37ClN2O5 |
| SMILES | O=C1N(CCCN(CCC2=CC=C(OC)C(OC)=C2)C)CCC3=CC(OC)=C(OC)C=C3C1.Cl |
1 Publications Citing Use of MCE
Summary
Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC 50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1 , HCN2 , HCN3 and HCN4 channels , with IC 50 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 K d 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 ED 50 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 100 mg/mL ( 202.82 mM ; Need ultrasonic)
DMSO : 100 mg/mL ( 202.82 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0282 mL | 10.1412 mL | 20.2823 mL |
| 5 mM | 0.4056 mL | 2.0282 mL | 4.0565 mL |
| 10 mM | 0.2028 mL | 1.0141 mL | 2.0282 mL |
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1.
Add each solvent one by one: PBS
Solubility: 110 mg/mL (223.11 mM); Clear solution; Need ultrasonic
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2.
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3.
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
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4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution
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.
- [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.
Synonyms