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  5. Histamine dihydrochloride

Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.

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

Histamine dihydrochloride Chemical Structure

Histamine dihydrochloride Chemical Structure

CAS No. : 56-92-8

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Based on 11 publication(s) in Google Scholar

Other Forms of Histamine dihydrochloride:

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Description

Histamine dihydrochloride is the agonist for histamine receptor and a vasodilator. Histamine dihydrochloride is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine dihydrochloride affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine dihydrochloride can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma[1][2][3][4][5][6][7].

In Vitro

Histamine dihydrochloride (0.01-10 μM, 72 h) exhibits a bidirectional regulatory effect on the proliferation of MDA-MB-231, arrests the cell cycle at G2/M phase, induces the formation of lipid droplet, induces differentiation and apoptosis in MDA-MB-231[4].
Histamine dihydrochloride (10 μM, 24 h) increases the generation of ROS, especially H2O2, reduces the activity of antioxidant enzymes (such as catalase), thereby promoting radiosensitivity in MDA-MB-231[4].
Histamine dihydrochloride (1-100 μM, 12 h) inhibits the migration of microglia and the release of inflammatory mediator IL-1β in LPS (HY-D1056)-stimulated N9 mouse microglial, exhibits anti-inflammatory activity[5].

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

Cell Proliferation Assay[4]

Cell Line: MDA-MB-231
Concentration: 0.01-10 µM
Incubation Time: 72 h
Result: Promoted cell proliferation at 10 µM, inhibited cell proliferation at 0.01 µM.

Apoptosis Analysis[4]

Cell Line: MDA-MB-231
Concentration: 10 µM
Incubation Time: 48 h
Result: Induced apoptosis.
In Vivo

Note:
Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

Histamine (0.05-100 μg/mouse, icv, single dose) exhibits analgesic effect at high doses of histamine (50-100 μg/mouse), causes hyperalgesia at low doses (0.1-1 μg/mouse) in mouse model[3].
Histamine dihydrochloride (62.5-2000 μg; Intravaginal injection) can exert a similar effect to estrogen in ovariectomized mice, causing a decrease in intravaginal tetrazolium, an increase in epithelial growth, and keratinization[6].
Histamine can be used in animal modeling to create gastrointestinal ulcer models[1].

Induction of Gastrointestinal Ulcer[1]
Background
Histamine can cause increased gastric acid secretion, decreased mucus production, reflux of pancreatic juice, poor gastric blood flow, and thus gastric ulcers. Stress can cause increased gastrointestinal motility, making the gastric folds more susceptible to damage when exposed to acid.
Specific Modeling Methods
Guinea Pig: male • albino • Administration: 5 mg/kg • i.p. • single dose
Note
(1) No eating or drinking is allowed 24 hours before the experiment.
(2) The animals are sacrificed 2 hours after histamine injection, and treated with 1% formalin to check for gastric ulcers.
Modeling Indicators
The ulcers were punctate or elongated. After the model was dissected, the ulcer index (the sum of the lengths of the lesions) was measured under a microscope to be 3.4 mm.
Correlated Product(s): Serotonin (HY-B1473A); Reserpine (HY-N0480)
Opposite Product(s): Cimetidine (HY-14289)

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

Animal Model: Ovariectomized female mice of the SW strain[6].
Dosage: 62.5-2000 μg
Administration: Intravaginal injection
Result: Stimulated a vaginal response similar to that caused by estrogen, resulting in a decrease in intravaginal tetrazolium, increased epithelial growth, and keratinization.
Animal Model: Mouse model[3].
Dosage: 0.05-100 μg/mouse
Administration: icv, single dose
Result: Prolonged the licking latency at the dose of 50 and 100 μg/mouse.
Shortened the licking latency at the dose of 0.1-1 μg/mouse.
Clinical Trial
Molecular Weight

184.07

Formula

C5H11Cl2N3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

NCCC1=CN=CN1.Cl.Cl

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°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 (543.27 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 5.4327 mL 27.1636 mL 54.3272 mL
5 mM 1.0865 mL 5.4327 mL 10.8654 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (13.58 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 (13.58 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: 100 mg/mL (543.27 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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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 +
+
%
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%
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

Purity: 99.68%

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 5.4327 mL 27.1636 mL 54.3272 mL 135.8179 mL
5 mM 1.0865 mL 5.4327 mL 10.8654 mL 27.1636 mL
10 mM 0.5433 mL 2.7164 mL 5.4327 mL 13.5818 mL
15 mM 0.3622 mL 1.8109 mL 3.6218 mL 9.0545 mL
20 mM 0.2716 mL 1.3582 mL 2.7164 mL 6.7909 mL
25 mM 0.2173 mL 1.0865 mL 2.1731 mL 5.4327 mL
30 mM 0.1811 mL 0.9055 mL 1.8109 mL 4.5273 mL
40 mM 0.1358 mL 0.6791 mL 1.3582 mL 3.3954 mL
50 mM 0.1087 mL 0.5433 mL 1.0865 mL 2.7164 mL
60 mM 0.0905 mL 0.4527 mL 0.9055 mL 2.2636 mL
80 mM 0.0679 mL 0.3395 mL 0.6791 mL 1.6977 mL
100 mM 0.0543 mL 0.2716 mL 0.5433 mL 1.3582 mL
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Histamine dihydrochloride
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