2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Fluparoxan

Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent.

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

Fluparoxan Chemical Structure

Fluparoxan Chemical Structure

CAS No. : 105182-45-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Other Forms of Fluparoxan:

Fluparoxan Related Antibodies

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α adrenergic receptor β adrenergic receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Fluparoxan is an orally active, selective and competitive alpha 2-adrenoceptor antagonist. Fluparoxan is an anti-depressant agent[1][2].

IC50 & Target

α2-adrenergic receptor

 

In Vitro

In the rat isolated, field-stimulated vas deferens and the guinea-pig isolated, field-stimulated ileum preparations, Fluparoxan is a reversible competitive antagonist of the inhibitory responses to the alpha 2-adrenoceptor agonist UK-14304 (HY-B0659) with pKB values of 7.87 and 7.89 respectively[1].
In the rat isolated anococcygeus muscle, Fluparoxan is a much weaker competitive antagonist of the contractile response to the alpha 1-adrenoceptor agonist phenylephrine (HY-B0769) with a pKB of 4.45 giving an alpha 2: alpha 1-adrenoceptor selectivity ratio of greater than 2500[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Fluparoxan Related Antibodies
In Vivo

In the conscious mouse, Fluparoxan (0.2-3.0 mg/kg) is effective by the oral route and of similar potency to idazoxan (HY-14561) in preventing clonidine (HY-12721)-induced hypothermia and antinociception[1].
Fluparoxan (0.67-6 mg/kg, p.o.) prevents UK-14304 (HY-B0659)-induced sedation and bradycardia in the dog[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

195.19

Formula

C10H10FNO2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C2C(O[C@]3([H])[C@@](CNC3)([H])O2)=CC=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (256.16 mM; Need ultrasonic; 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 5.1232 mL 25.6161 mL 51.2321 mL
5 mM 1.0246 mL 5.1232 mL 10.2464 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. 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (12.81 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 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (12.81 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)

g

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).
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
References

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.1232 mL 25.6161 mL 51.2321 mL 128.0803 mL
5 mM 1.0246 mL 5.1232 mL 10.2464 mL 25.6161 mL
10 mM 0.5123 mL 2.5616 mL 5.1232 mL 12.8080 mL
15 mM 0.3415 mL 1.7077 mL 3.4155 mL 8.5387 mL
20 mM 0.2562 mL 1.2808 mL 2.5616 mL 6.4040 mL
25 mM 0.2049 mL 1.0246 mL 2.0493 mL 5.1232 mL
30 mM 0.1708 mL 0.8539 mL 1.7077 mL 4.2693 mL
40 mM 0.1281 mL 0.6404 mL 1.2808 mL 3.2020 mL
50 mM 0.1025 mL 0.5123 mL 1.0246 mL 2.5616 mL
60 mM 0.0854 mL 0.4269 mL 0.8539 mL 2.1347 mL
80 mM 0.0640 mL 0.3202 mL 0.6404 mL 1.6010 mL
100 mM 0.0512 mL 0.2562 mL 0.5123 mL 1.2808 mL
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Fluparoxan Related Classifications

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.

Keywords:

Fluparoxan105182-45-4GR50360GR 50360GR-50360Adrenergic ReceptorBeta Receptoralpha 2-adrenoceptororally activeInhibitorinhibitorinhibit

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