LKT Labs

Biochemicals for Life Science Research

Efaroxan Hydrochloride

Product ID E2002
Cas No. 89197-00-2
Purity ≥99%
Product Unit SizeCostQuantityStock
25 mg $116.50 In stock
100 mg $297.60 In stock
250 mg $658.00 In stock
Bulk Quote

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Description

Efaroxan hydrochloride is an antagonist at α2-adrenergic receptors and imidazoline-1 receptors. Efaroxan hydrochloride administration in animal models of opioid use shows a potential role for α2-adrenergic receptors in opioid-mediated mechanisms of tolerance and antinociception. This compound also exhibits antihyperglycemic activity, improving oral glucose tolerance in animal models of diabetes due to its ability to inhibit K(ATP) K+ channels on pancreatic beta cells. Additionally, administration of efaroxan hydrochloride shows benefit in animal models of Parkinson’s Disease.

Product Info

Cas No.

89197-00-2
Purity

≥99%
Formula

C13H16N2O • HCl
Formula Wt.

252.74
IUPAC Name

2-(2-ethyl-3H-1-benzofuran-2-yl)-4,5-dihydro-1H-imidazole;hydrochloride
Melting Point

250°C
Solubility

Soluble to 100 mM in water
Appearance

White powder

Shipping and Storage

Store Temp

Ambient
Ship Temp

Ambient

Downloads

MSDS

E2002 MSDS PDF
Info Sheet

E2002 Info Sheet PDF

References

Milne B, Jhamandas K, Sutak M, et al. Stereo-selective inhibition of spinal morphine tolerance and hyperalgesia by an ultra-low dose of the alpha-2-adrenoceptor antagonist efaroxan. Eur J Pharmacol. 2013 Feb 28;702(1-3):227-34. PMID: 23376415.

Lehner Z, Stadlbauer K, Adorjan I, et al. Mechanisms of antihyperglycaemic action of efaroxan in mice: time for reappraisal of α2A-adrenergic antagonism in the treatment of type 2 diabetes? Diabetologia. 2012 Nov;55(11):3071-82. PMID: 22898767.

Le Brigand L, Virsolvy A, Manechez D, et al. In vitro mechanism of action on insulin release of S-22068, a new putative antidiabetic compound. Br J Pharmacol. 1999 Nov;128(5):1021-6. PMID: 10556939.

Chopin P, Colpaert FC, Marien M. Effects of alpha-2 adrenoceptor agonists and antagonists on circling behavior in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal pathway. J. Pharmacol. Exp. Ther. 1999. 288 (2): 798–804. PMID 9918591.

Chan SL, Dunne MJ, Stillings MR, et al. The alpha 2-adrenoceptor antagonist efaroxan modulates K+ATP channels in insulin-secreting cells. Eur J Pharmacol. 1991 Oct 29;204(1):41-8. PMID: 1687123.

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