[CAS NO. 89197-00-2] Efaroxan hydrochloride
PRODUCTS SPECIFICATIONS [89197-00-2]
DESCRIPTION [89197-00-2]
Overview
| MDL | MFCD00069270 |
|---|---|
| Molecular Weight | 252.74 |
| Molecular Formula | C13H17ClN2O |
| SMILES | CCC1(C2=NCCN2)OC3=CC=CC=C3C1.[H]Cl |
Summary
Efaroxan hydrochloride is a potent, selective and orally active α2-adrenoceptor antagonist, with antidiabetic activity. Efaroxan hydrochloride is a selective I1-Imidazoline receptor antagonist. Efaroxan hydrochloride can be used for the research of cardiovascular disease [1] [2] [3] .
In Vitro
Efaroxan hydrochloride binds to I1-imidazoline and α2-adrenergic receptors in bovine rostral ventrolateral medulla membranes, with K i s of 0.15 nM and 5.6 nM, respectively [1]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Efaroxan hydrochloride increases plasma insulin levels in both conscious fed and fasted rats without greatly affecting plasma glucoselevels
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley rats (weight range 250-300g) [3] |
| Dosage: | 1 mg/kg, 5 mg/kg |
| Administration: | Oral administration |
| Result: | Produced a significant increase in plasma insulin levels of starved rats 15 and 30 min after treatment. |
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
DMSO : 50 mg/mL ( 197.83 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.9566 mL | 19.7832 mL | 39.5664 mL |
| 5 mM | 0.7913 mL | 3.9566 mL | 7.9133 mL |
| 10 mM | 0.3957 mL | 1.9783 mL | 3.9566 mL |
References
- [1] T L Berridge, et al. Selectivity profile of the alpha 2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat. Eur J Pharmacol. 1992 Mar 24;213(2):205-12.
- [2] A O Abdel-Zaher, et al. The potential antidiabetic activity of some alpha-2 adrenoceptor antagonists. Pharmacol Res. 2001 Nov;44(5):397-409.
- [3] T L Berridge, et al. Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats. Eur J Pharmacol. 1992 Mar 24;213(2):213-8.