Efaroxan hydrochloride

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Cat.No. 0792 - Efaroxan hydrochloride | C13H16N2O.HCl | CAS No. 89197-00-2
Description: α2 antagonist and I1, I3 ligand
Chemical Name: 2-(2-Ethyl-2,3-dihydro-2-benzofuranyl)-4,5-dihydro-1H-imidazole hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

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

SolubilitySoluble 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

Certificate of Analysis is currently unavailable
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Safety Datasheet

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


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Citations for Efaroxan hydrochloride

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