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

Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder.

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

Hydroxyzine Chemical Structure

Hydroxyzine Chemical Structure

CAS No. : 68-88-2

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100 mg USD 65 In-stock
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Other Forms of Hydroxyzine:

Hydroxyzine Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder[1].

IC50 & Target[1]

H1 Receptor

 

Cellular Effect
Cell Line Type Value Description References
Huh-7 CC50
42.6 μM
Compound: Rac-5
Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis
Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis
[PMID: 26599718]
In Vitro

Hydroxyzine dihydrochloride inhibits carbachol (10 μM)-induced serotonin release by 34% at 10 μM, by 25% 1 μM and by 17% 0.1 μM in pretreated bladder slices for 60 min[1].

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

Hydroxyzine Related Antibodies
In Vivo

Hydroxyzine dihydrochloride (12.5 mg/kg, 25 mg/kg and 50 mg/kg i.p.) shows little direct analgesic activity but markedly potentiates only the effect of morphine on the vocalization after-discharge which represents the affective component of pain in rats. Hydroxyzine dihydrochloride (50 mg/kg i.p.) potentiates morphine on the tail-flick test, while Hydroxyzine (12.5 mg/kg i.p.) decreases morphine antinociception in rats[3].

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

374.90

Formula

C21H27ClN2O2
CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

ClC1=CC=C(C(N2CCN(CCOCCO)CC2)C3=CC=CC=C3)C=C1
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 : 100 mg/mL (266.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (13.34 mM; ultrasonic and warming and adjust pH to 4 with HCl and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6674 mL 13.3369 mL 26.6738 mL
5 mM 0.5335 mL 2.6674 mL 5.3348 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 (6.67 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.67 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).

*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
H2O / DMSO 1 mM 2.6674 mL 13.3369 mL 26.6738 mL 66.6845 mL
5 mM 0.5335 mL 2.6674 mL 5.3348 mL 13.3369 mL
10 mM 0.2667 mL 1.3337 mL 2.6674 mL 6.6684 mL
DMSO 15 mM 0.1778 mL 0.8891 mL 1.7783 mL 4.4456 mL
20 mM 0.1334 mL 0.6668 mL 1.3337 mL 3.3342 mL
25 mM 0.1067 mL 0.5335 mL 1.0670 mL 2.6674 mL
30 mM 0.0889 mL 0.4446 mL 0.8891 mL 2.2228 mL
40 mM 0.0667 mL 0.3334 mL 0.6668 mL 1.6671 mL
50 mM 0.0533 mL 0.2667 mL 0.5335 mL 1.3337 mL
60 mM 0.0445 mL 0.2223 mL 0.4446 mL 1.1114 mL
80 mM 0.0333 mL 0.1667 mL 0.3334 mL 0.8336 mL
100 mM 0.0267 mL 0.1334 mL 0.2667 mL 0.6668 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Hydroxyzine 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:

Hydroxyzine68-88-2Histamine ReceptoritchingnauseaanxietytensionGADdisorderInhibitorinhibitorinhibit

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