1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Methapyrilene hydrochloride

Methapyrilene hydrochloride  (Synonyms: Thenylpyramine hydrochloride)

Cat. No.: HY-B1483 Purity: 99.88%
Handling Instructions Technical Support

Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo

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

Methapyrilene hydrochloride Chemical Structure

Methapyrilene hydrochloride Chemical Structure

CAS No. : 135-23-9

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Other Forms of Methapyrilene hydrochloride:

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Description

Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo[2]

IC50 & Target[1]

H1 Receptor

 

In Vitro

Methapyrilene hydrochloride (650 μM) results in a down-regulation of TF and up-regulation of FTL, while the level of HMOX1 is not changed. Additionally, the levels of CD44 and SOX9 proteins and the expression of PROM1 (CD133), hepatic stem cell-associated markers are increased[1].
Methapyrilene hydrochloride (650 μM) decreases CYP2E1, CYP3A4, NR1l3, ALB, mRNA expression and increases CD133 expression[1].

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

In Vivo

Methapyrilene hydrochloride (oral gavage; 40 or 80 mg/kg; 5 days per week; 6 weeks) results in changes in the expression of classic hepatotoxicity-related marker genes and iron homeostasis-related genes, especially a prominent, dose-dependent down-regulation of the transferrin (Tf) gene and an up-regulation of the ferritin, light chain (FTL) gene in rats[1].
Methapyrilene hydrochloride (oral gavage; 150 mg/kg; 3 days) causes periportal liver necrosis at high dosage. Methapyrilene is sufficient to induce liver necrosis, or a subtoxic dose of 50 mg/kg/day[2].

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

Molecular Weight

297.85

Formula

C14H20ClN3S

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

CN(C)CCN(C1=NC=CC=C1)CC2=CC=CS2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (335.74 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 3.3574 mL 16.7870 mL 33.5739 mL
5 mM 0.6715 mL 3.3574 mL 6.7148 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 (sealed storage, away from moisture). 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 (8.39 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 (8.39 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 (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 3.3574 mL 16.7870 mL 33.5739 mL 83.9349 mL
5 mM 0.6715 mL 3.3574 mL 6.7148 mL 16.7870 mL
10 mM 0.3357 mL 1.6787 mL 3.3574 mL 8.3935 mL
15 mM 0.2238 mL 1.1191 mL 2.2383 mL 5.5957 mL
20 mM 0.1679 mL 0.8393 mL 1.6787 mL 4.1967 mL
25 mM 0.1343 mL 0.6715 mL 1.3430 mL 3.3574 mL
30 mM 0.1119 mL 0.5596 mL 1.1191 mL 2.7978 mL
40 mM 0.0839 mL 0.4197 mL 0.8393 mL 2.0984 mL
50 mM 0.0671 mL 0.3357 mL 0.6715 mL 1.6787 mL
60 mM 0.0560 mL 0.2798 mL 0.5596 mL 1.3989 mL
80 mM 0.0420 mL 0.2098 mL 0.4197 mL 1.0492 mL
100 mM 0.0336 mL 0.1679 mL 0.3357 mL 0.8393 mL
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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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Methapyrilene hydrochloride
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