Biological Activity
Potent, highly selective α2 adrenoceptor antagonist and imidazoline I1 receptor ligand (pKi values are 7.87, 7.42, 5.74, 7.28 and < 5 for α 2A, α2B, α2C, I1, and I2 receptors respectively). Promotes insulin secretion, at a site distinct from I1 or I2 (the putative I3 receptor) in vitro and in vivo.
Technical Data
| M. Wt | 252.74 |
| Formula | C13H16N2O.HCl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 89197-00-2 |
| PubChem ID | 11957548 |
| InChI Key | DWOIUCRHVWIHAH-UHFFFAOYSA-N |
| Smiles | Cl.CCC1(CC2=CC=CC=C2O1)C1=NCCN1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 100 mM in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 252.74. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.96 mL | 19.78 mL | 39.57 mL |
| 5 mM | 0.79 mL | 3.96 mL | 7.91 mL |
| 10 mM | 0.4 mL | 1.98 mL | 3.96 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.79 mL |
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Product Datasheets
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References
References are publications that support the products' biological activity.
Chapleo et al (1984) α-Adrenoceptor reagents 2. Effects of modification of the 1,4-benzodioxan ring system on α-adrenoceptor activity. J.Med.Chem. 27 570 PMID: 6143826
Eglen et al (1998) 'Seeing through a glass darkly': casting light on imidazoline 'I' sites. TiPS 19 381 PMID: 9786027
Mayer and Taberner (2002) Effects of the imidazoline ligands efaroxan and KU14R on blood glucose in the mouse. Eur.J.Pharmacol. 454 95 PMID: 12409010
Olmos et al (1994) Imidazolines stimulate release of insulin from RIN-5AH cells independently from imidazoline I1 and I2 receptors. Eur.J.Pharmacol. 262 41 PMID: 7813577
Keywords: Efaroxan hydrochloride, supplier, α2-adrenoceptor, alpha2-adrenoceptor, a2-adrenoceptor, α2-Adrenergic, alpha2-Adrenergic, a2-adrenergic, antagonists, I1, I3, ligand, Receptors, General, Imidazolines, Adrenergic, Alpha-2, Receptors, General, Imidazolines, Adrenergic, Alpha-2, Receptors, Tocris Bioscience
