Efaroxan hydrochloride

Name: Efaroxan hydrochloride
Brand: MedChemExpress
SKU: HY-B1416A
Rating: 4.5 (1 reviews)

Cat. No.: HY-B1416A Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 89197-00-2

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 70	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

α adrenergic receptor

In Vitro

Efaroxan hydrochloride binds to I1-imidazoline and α2-adrenergic receptors in bovine rostral ventrolateral medulla membranes, with K_is of 0.15 nM and 5.6 nM, respectively^[1]

MedChemExpress (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].

MedChemExpress (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.

89197-00-2

Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.94%

Select Batch:

Data Sheet (278 KB) SDS (420 KB)

COA (254 KB) RP-HPLC (210 KB) MS (175 KB)

Handling Instructions (2659 KB)

References

[1]. Berridge TL, et al. Selectivity profile of the alpha 2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat. Eur J Pharmacol. 1992 Mar 24;213(2):205-12. [Content Brief]

[2]. T L Berridge, et al. Selectivity profile of the alpha 2-adrenoceptor antagonist efaroxan in relation to plasma glucose and insulin levels in the rat. Eur J Pharmacol. 1992 Mar 24;213(2):205-12.

[3]. A O Abdel-Zaher, et al. The potential antidiabetic activity of some alpha-2 adrenoceptor antagonists. Pharmacol Res. 2001 Nov;44(5):397-409. [Content Brief]

[4]. T L Berridge, et al. Comparison of the effects of efaroxan and glibenclamide on plasma glucose and insulin levels in rats. Eur J Pharmacol. 1992 Mar 24;213(2):213-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.9566 mL	19.7832 mL	39.5664 mL	98.9159 mL
	5 mM	0.7913 mL	3.9566 mL	7.9133 mL	19.7832 mL
	10 mM	0.3957 mL	1.9783 mL	3.9566 mL	9.8916 mL
	15 mM	0.2638 mL	1.3189 mL	2.6378 mL	6.5944 mL
	20 mM	0.1978 mL	0.9892 mL	1.9783 mL	4.9458 mL
	25 mM	0.1583 mL	0.7913 mL	1.5827 mL	3.9566 mL
	30 mM	0.1319 mL	0.6594 mL	1.3189 mL	3.2972 mL
	40 mM	0.0989 mL	0.4946 mL	0.9892 mL	2.4729 mL
	50 mM	0.0791 mL	0.3957 mL	0.7913 mL	1.9783 mL
	60 mM	0.0659 mL	0.3297 mL	0.6594 mL	1.6486 mL
	80 mM	0.0495 mL	0.2473 mL	0.4946 mL	1.2364 mL
	100 mM	0.0396 mL	0.1978 mL	0.3957 mL	0.9892 mL