2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Antazoline

Antazoline  (Synonyms: Phenazoline)

Cat. No.: HY-B1067A Purity: 99.70%
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Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect.

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

Antazoline Chemical Structure

Antazoline Chemical Structure

CAS No. : 91-75-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Antazoline:

Antazoline Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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Description

Antazoline (Phenazoline) is an H1 receptor antagonist that affects the activity of the central nervous system, has a potent antiarrhythmic effect[1][2][3].

IC50 & Target

H1 Receptor

 

In Vitro

Antazoline (Phenazoline) shows good inhibitory effect on HBV DNA in the supernatant of HepAD38 and Huh7 cells with the value of EC50 is 2.910 μmol/L and 2.349 μmol/L, respectively[2].

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

Antazoline Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: HepAD38 cells
Concentration: 10μmol/L
Incubation Time: 5 days
Result: Exhibited no significant cytotoxicity at a concentration of 10μmol/L and had a dose-dependent inhibition of HBV DNA in the supernatant.

RT-PCR[2]

Cell Line: Huh7 cells
Concentration: 30 μmol/L, 10 μmol/L, 3.33 μmol/L, 1.1 μmol/L, 0.370 μmol/L, and 0.123 μmol/L
Incubation Time: 4 days
Result: Had a significant inhibitory effect on HBV DNA in supernatants in a dose-dependent manner.
In Vivo

Antazoline (IP; 0.01 ml/g; 30min) as H1 receptor antagonists diminishes the anticonvulsant activity of carbamazepine and diphenylhydantoin[3].

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

Animal Model: Swiss mice[3]
Dosage: 0.01 mL/g
Administration: Antazoline (IP; 0.01 ml/g; 30min)
Result: Showed some proconvulsive activity.
Clinical Trial
Molecular Weight

265.35

Formula

C17H19N3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(CN(C2=CC=CC=C2)CC3=CC=CC=C3)=NCCN1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (188.43 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 3.7686 mL 18.8430 mL 37.6861 mL
5 mM 0.7537 mL 3.7686 mL 7.5372 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 (protect from light). 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.42 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 (9.42 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 3.7686 mL 18.8430 mL 37.6861 mL 94.2152 mL
5 mM 0.7537 mL 3.7686 mL 7.5372 mL 18.8430 mL
10 mM 0.3769 mL 1.8843 mL 3.7686 mL 9.4215 mL
15 mM 0.2512 mL 1.2562 mL 2.5124 mL 6.2810 mL
20 mM 0.1884 mL 0.9422 mL 1.8843 mL 4.7108 mL
25 mM 0.1507 mL 0.7537 mL 1.5074 mL 3.7686 mL
30 mM 0.1256 mL 0.6281 mL 1.2562 mL 3.1405 mL
40 mM 0.0942 mL 0.4711 mL 0.9422 mL 2.3554 mL
50 mM 0.0754 mL 0.3769 mL 0.7537 mL 1.8843 mL
60 mM 0.0628 mL 0.3141 mL 0.6281 mL 1.5703 mL
80 mM 0.0471 mL 0.2355 mL 0.4711 mL 1.1777 mL
100 mM 0.0377 mL 0.1884 mL 0.3769 mL 0.9422 mL
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Antazoline 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:

Antazoline91-75-8PhenazolineHistamine ReceptorH1 receptor antagonistnervous systemInhibitorinhibitorinhibit

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