1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
    Imidazoline Receptor
  3. Efaroxan hydrochloride

Efaroxan hydrochloride 

Cat. No.: HY-B1416A Purity: 99.94%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Efaroxan hydrochloride Chemical Structure

Efaroxan hydrochloride Chemical Structure

CAS No. : 89197-00-2

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Based on 1 publication(s) in Google Scholar

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Description

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].

IC50 & Target

α2-adrenoceptor, I1-Imidazoline receptor[1][2]

In Vitro

Efaroxan hydrochloride binds to I1-imidazoline and α2-adrenergic receptors in bovine rostral ventrolateral medulla membranes, with Kis 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.
Molecular Weight

252.74

Formula

C13H17ClN2O

CAS No.
SMILES

CCC1(C2=NCCN2)OC3=CC=CC=C3C1.[H]Cl

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
In Vitro: 

DMSO : 50 mg/mL (197.83 mM; ultrasonic and warming and heat to 60°C)

Preparing
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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.94%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Efaroxan hydrochloride
Cat. No.:
HY-B1416A
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