[CAS NO. 85175-67-3] Zatebradine
PRODUCTS SPECIFICATIONS [85175-67-3]
DESCRIPTION [85175-67-3]
Overview
| MDL | MFCD00867014 |
|---|---|
| Molecular Weight | 456.57 |
| Molecular Formula | C26H36N2O5 |
| SMILES | O=C1N(CCCN(CCC2=CC=C(OC)C(OC)=C2)C)CCC3=CC(OC)=C(OC)C=C3C1 |
1 Publications Citing Use of MCE
Summary
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 IC 50 value of 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
Oil
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
Ethanol : 100 mg/mL ( 219.02 mM ; Need ultrasonic)
DMSO : ≥ 50 mg/mL ( 109.51 mM )
* "≥" means soluble, but saturation unknown.
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 |
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.