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.
|Storage||Store at RT|
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||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|
The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.
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
If you know of a relevant reference for Efaroxan hydrochloride, please let us know.
View Related Products by Target
View Related Products by Product Action
Keywords: α2-adrenoceptor alpha2-adrenoceptor a2-adrenoceptor α2-Adrenergic alpha2-Adrenergic a2-adrenergic antagonists I1 I3 ligand Receptors General Imidazolines Adrenergic Alpha-2 Receptors
Citations for Efaroxan hydrochloride
Citations are publications that use Tocris products.
Currently there are no citations for Efaroxan hydrochloride. Do you know of a great paper that uses Efaroxan hydrochloride from Tocris? If so please let us know.
Literature in this Area
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.