2. GPCR/G Protein Neuronal Signaling Anti-infection
  3. 5-HT Receptor SARS-CoV
  4. Azaperone dimaleate

Azaperone dimaleate  (Synonyms: Quipazine dimaleate)

Cat. No.: HY-101046 Purity: 99.87%
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Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research.

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Azaperone dimaleate Chemical Structure

Azaperone dimaleate Chemical Structure

CAS No. : 150323-78-7

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Based on 1 publication(s) in Google Scholar

Other Forms of Azaperone dimaleate:

Azaperone dimaleate Related Antibodies

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Description

Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research[1][2][3][4].

In Vitro

Quipazine dimaleate shows binding efficacy to 5-HT1 and 5-HT2 with Ki values of 230 nM[3].
Quipazine dimaleate displaces [3H]GR65630 from 5-HT3R in rat entorhinal cortex with a Ki value of 1.4 nM[3].
Quipazine dimaleate shows antagonistic properties on the rat vagus nerve with pIC50 value of 6.1, 6.49 and 6.17 for 5-HT2, 5-HT1 and inhibition of 5-HT release[4].

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

Azaperone dimaleate Related Antibodies
In Vivo

Quipazine dimaleate (2.5, 5 and 7.5 mg/kg, one dose for once; i.p.) affects dietary self-selection of different macronutrient diets in male and female rats[1].

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

Animal Model: Male and female Wistar rats feed with different sources of the three macronutrients (Group 1: casein, corn starch, safflower oil. Group 2: egg protein, corn starch/sucrose, lard. Group S: casein hydrolysate, maltose dextrin, butter.)[1]
Dosage: 2.5, 5 and 7.5 mg/kg
Administration: Intraperitoneal injection; 2.5, 5 and 7.5 mg/kg, one dose for once
Result: Increased water intake and food intake of male rats from Group S, and reduced food intake of female rats from Group 1 and Group 2s at 2h post-injection. Reduced food intake in female rats from Group 2, reduced protein intake in female rats from Group 1.
Molecular Weight

445.42

Formula

C21H23N3O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)/C=C\C(O)=O.O=C(O)/C=C\C(O)=O.C1(N2CCNCC2)=NC3=CC=CC=C3C=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 : 250 mg/mL (561.27 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 2.2451 mL 11.2254 mL 22.4507 mL
5 mM 0.4490 mL 2.2451 mL 4.4901 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.

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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: ≥ 2.08 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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 2.2451 mL 11.2254 mL 22.4507 mL 56.1268 mL
5 mM 0.4490 mL 2.2451 mL 4.4901 mL 11.2254 mL
10 mM 0.2245 mL 1.1225 mL 2.2451 mL 5.6127 mL
15 mM 0.1497 mL 0.7484 mL 1.4967 mL 3.7418 mL
20 mM 0.1123 mL 0.5613 mL 1.1225 mL 2.8063 mL
25 mM 0.0898 mL 0.4490 mL 0.8980 mL 2.2451 mL
30 mM 0.0748 mL 0.3742 mL 0.7484 mL 1.8709 mL
40 mM 0.0561 mL 0.2806 mL 0.5613 mL 1.4032 mL
50 mM 0.0449 mL 0.2245 mL 0.4490 mL 1.1225 mL
60 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9354 mL
80 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7016 mL
100 mM 0.0225 mL 0.1123 mL 0.2245 mL 0.5613 mL
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Azaperone dimaleate 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:

Azaperone dimaleate150323-78-7Quipazine dimaleate5-HT ReceptorSARS-CoVSerotonin Receptor5-hydroxytryptamine ReceptorSARS coronavirusantiviralneurological diseaseGR65630rat vagus nerveentorhinal cortexmacronutrient dietInhibitorinhibitorinhibit

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