1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor mAChR Adrenergic Receptor
  3. Promethazine hydrochloride

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.

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

Promethazine hydrochloride Chemical Structure

Promethazine hydrochloride Chemical Structure

CAS No. : 58-33-3

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Based on 1 publication(s) in Google Scholar

Other Forms of Promethazine hydrochloride:

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors[1][2].

IC50 & Target

H1 Receptor

 

In Vitro

Promethazine hydrochloride (1.25-10 μM, 3 days) inhibits adipocyte formation in a dose-dependent manner[1].
Promethazine hydrochloride (10 μM, 0-12 days) decreases the expression of peroxisome proliferator activated receptor γ (PPARG) and reduces the phosphorylation level of CREB in PDGFRα+ cells[1].
Promethazine hydrochloride (10-1000 μM, 1-24 h) has cytotoxic at concentrations greater than 100 μM in L929 lung fibroblast cells[3].

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

In Vivo

Promethazine hydrochloride (0.05-0.1 mg/mL, p.o., 4 weeks) possesses inhibitory effect on ectopic fat cell formation in skeletal muscle in a mouse achilles tendon rupture model[1].
Promethazine hydrochloride (2.4-9.6 mg/kg, p.o.) has no effect on the development of femoral osteoporosis and retarded normal femoral expansion in the adult castrate male rats[4].

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

Clinical Trial
Molecular Weight

320.88

Formula

C17H21ClN2S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC(N(C)C)CN1C(C=CC=C2)=C2SC3=CC=CC=C13.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*The compound is unstable in solutions, freshly prepared is recommended.

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (311.64 mM; Need ultrasonic)

DMSO : 50 mg/mL (155.82 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 3.1164 mL 15.5821 mL 31.1643 mL
5 mM 0.6233 mL 3.1164 mL 6.2329 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

* 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 (7.79 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 (7.79 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 120 mg/mL (373.97 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 3.1164 mL 15.5821 mL 31.1643 mL 77.9107 mL
5 mM 0.6233 mL 3.1164 mL 6.2329 mL 15.5821 mL
10 mM 0.3116 mL 1.5582 mL 3.1164 mL 7.7911 mL
15 mM 0.2078 mL 1.0388 mL 2.0776 mL 5.1940 mL
20 mM 0.1558 mL 0.7791 mL 1.5582 mL 3.8955 mL
25 mM 0.1247 mL 0.6233 mL 1.2466 mL 3.1164 mL
30 mM 0.1039 mL 0.5194 mL 1.0388 mL 2.5970 mL
40 mM 0.0779 mL 0.3896 mL 0.7791 mL 1.9478 mL
50 mM 0.0623 mL 0.3116 mL 0.6233 mL 1.5582 mL
60 mM 0.0519 mL 0.2597 mL 0.5194 mL 1.2985 mL
80 mM 0.0390 mL 0.1948 mL 0.3896 mL 0.9739 mL
100 mM 0.0312 mL 0.1558 mL 0.3116 mL 0.7791 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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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.

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Promethazine hydrochloride
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HY-B0781
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