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Gastrointestinal Inflammation and Ulcer Models Gastrointestinal Disease Models
Gastric Ulcer Models Duodenal Ulcer Models
Histamine dihydrochloride

Cat. No.: HY-B0722

Histamine dihydrochloride

21 Cited Publications

Customer Review

Based on 21 publication(s) in Google Scholar

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.

Purity: 99.92%
CAS No.: 56-92-8
Formula: C₅H₁₁Cl₂N₃
Molecular Weight:184.07

Storage:

4°C, sealed storage, away from moisture

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

Histamine dihydrochloride Chemical Structure

CAS No.: 56-92-8

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Induced Disease Models
Chemical Information
Publications (21)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Histamine Receptor Isoforms :

All Akt Isoforms :

All Endogenous Metabolite Isoforms :

All p38 MAPK Isoforms :

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

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.

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.

Induced Disease Models

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.

Chemical Information

CAS No. 56-92-8
Appearance Solid
Molecular Weight 184.07
Formula C₅H₁₁Cl₂N₃
Color Light yellow to brown
SMILES

NCCC1=CN=CN1.Cl.Cl
Structure Classification
- Others
Initial Source
- Endogenous metabolite
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)

Publications (21)

All In Vivo Efficacy StudyRT-PCRIFWB

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Journal Impact Factor

Cancer Cell

Cancer cell autophagy, reprogrammed macrophages, and remodeled vasculature in glioblastoma triggers tumor immunity. [Abstract]

2022 Oct 10;40(10):1111-1127.e9. PMID: 36113478
Immunity

Spatiotemporal dynamics of CXCL10 encode contextual immune information revealed by the genetically encoded fluorescent sensor. [Abstract]

2025 Sep 9;58(9):2320-2335.e9. PMID: 40818452
Adv Sci (Weinh)

MCU Upregulation Overactivates Mitophagy by Promoting VDAC1 Dimerization and Ubiquitination in the Hepatotoxicity of Cadmium. [Abstract]

2023 Mar;10(7):e2203869. PMID: 36642847

Histamine dihydrochloride purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2203869. [Abstract]

Confocal microscopy of mitochondrial Ca²⁺ levels in HepG2 transfected with GCaMP6m. Histamine (100 μM) was applied to stimulate mitochondrial Ca²⁺ accumulation, and the 475/410 fluorescence ratio was analyzed.
Gut Microbes

Aging-caused the changes of the gut microbiota drive intestinal barrier dysfunction and increase sepsis susceptibility. [Abstract]

2026 Dec 31;18(1):2630475. PMID: 41723572
ACS Sens

A Sensitive Green-Red FRET Sensor for Calpain-1 Utilizing Heterodimeric Fluorescent Proteins from Distinct Evolutionary Origins. [Abstract]

2026 Mar 27;11(3):1891-1907. PMID: 41837894
Br J Pharmacol

A plant-derived TRPV3 inhibitor suppresses pain and itch. [Abstract]

2021 Apr;178(7):1669-1683. PMID: 33501656
J Agric Food Chem

Bifidobacterium animalis Subsp. Lactis Bla36 Postbiotics Ameliorate Allergic Rhinitis in Juvenile Mice by Repairing the Mucosal Barrier and Modulating Inflammatory Pathways. [Abstract]

2025 Nov 19;73(46):29604-29618. PMID: 41199139
Front Pharmacol

Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. [Abstract]

2019 Nov 15;10:1380. PMID: 31824317

Histamine dihydrochloride purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2019 Nov 15;10:1380. [Abstract]

Effects of histamine (0.1%, 20 µL/site, intradermal injection) on scratching behavior in mice.
mBio

Mycobacterium tuberculosis Utilizes Host Histamine Receptor H1 to Modulate Reactive Oxygen Species Production and Phagosome Maturation via the p38MAPK-NOX2 Axis. [Abstract]

2022 Oct 26;13(5):e0200422. PMID: 36000734
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
FASEB J

MRGPRX2 Mediates Mast Cell-Induced Endometriosis Pain Through the Sensitization of Sensory Neurons via Histamine/HRH1/TRPV1 Signaling Pathway. [Abstract]

2025 Jul 15;39(13):e70778. PMID: 40600649

Histamine dihydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Changes in HRH1 gene expression in F11 cells after treatment with 10⁻⁷ mM histamine for 24 h, as measured by RT–qPCR.

Histamine dihydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Changes in HRH1 protein expression in F11 cells after treatment with 10⁻⁷ mM histamine for 24 h, as detected by western blotting.

Histamine dihydrochloride purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]

Increase in the Ca²⁺ peak (DF/F0) in F11 cells from the control, histamine (10⁻⁷ mM for 24 h), and histamine+DLT groups (n = 3 in each group).
Toxics

Co-Exposure of Microplastics and Avermectin at Environmental-Related Concentrations Caused Severe Heart Damage Through ROS-Mediated MAPK Signaling in Larval and Adult Zebrafish. [Abstract]

2025 Dec 25;14(1):24. PMID: 41600573
J Cell Commun Signal

Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis. [Abstract]

2023 Mar;17(1):151-165. PMID: 36284029
Microbiol Spectr

Disruption of the Intestinal Mucosal Barrier Induced by High Fructose and Restraint Stress Is Regulated by the Intestinal Microbiota and Microbiota Metabolites. [Abstract]

2023 Jan 31;11(2):e0469822. PMID: 36719201
Insect Sci

UV2 and LW opsin genes mediate phototactic responses in the Asian lady beetle, Harmonia axyridis. [Abstract]

2025 Sep 11. PMID: 40931758
Fishes

2025 Aug 14.
Biochem Biophys Res Commun

TRPC1 downregulation enhances catecholamine secretion in adrenal chromaffin cells under metabolic syndrome conditions. [Abstract]

2025 Apr 1:755:151566. PMID: 40043610
Biol Pharm Bull

Inhibition of TRPC4/5 Channel Is Effective in Protecting against Histamine-Induced Hyperpermeability by Blocking Ca2+ Influx in Lung Microvascular Endothelial Cells. [Abstract]

2023;46(6):864-868. PMID: 37258152
bioRxiv

2026 Mar 30.
JID Innov

The PAR2 Antagonist Larazotide Can Mitigate Acute Histamine-Stimulated Epithelial Barrier Disruption in Keratinocytes: A Potential Adjunct Treatment for Atopic Dermatitis. [Abstract]

2025 Apr 3;5(4):100369. PMID: 40330848
bioRxiv

2024 June 12.

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.4327 mL

27.1636 mL

54.3272 mL

5 mM

1.0865 mL

5.4327 mL

10.8654 mL

10 mM

0.5433 mL

2.7164 mL

5.4327 mL

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

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

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Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (13.58 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.

Working Solution

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:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (286 KB)
SDS (558 KB)
- English - EN (558 KB)
- Français - FR (558 KB)
- Deutsch - DE (558 KB)
- Norwegian - NO (558 KB)
- Español - ES (558 KB)
- Swedish - SV (558 KB)
- Italian - IT (558 KB)
- Korean - KR (558 KB)
- Portuguese - PT (558 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Okabe S, et al. Effects of cimetidine, a histamine H2-receptor antagonist, on various experimental gastric and duodenal ulcers. Am J Dig Dis. 1977 Aug;22(8):677-84. [Content Brief]

[2]. Rietveld S et al. The influence of respiratory sounds on breathlessness in children with asthma: a symptom-perceptionapproach. Health Psychol. 1997 Nov;16(6):547-53. [Content Brief]

[3]. Malmberg-Aiello P, et al., Role of histamine in rodent antinociception. Br J Pharmacol. 1994 Apr;111(4):1269-79. [Content Brief]

[4]. Medina V, et al., Histamine-mediated signaling processes in human malignant mammary cells. Cancer Biol Ther. 2006 Nov;5(11):1462-71. [Content Brief]

[5]. Ferreira R, et al., Histamine modulates microglia function. J Neuroinflammation. 2012 May 8;9:90. [Content Brief]

[6]. MARTIN L. The effects of histamine on the vaginal epithelium of the mouse. J Endocrinol. 1962 Jan;23:329-40. [Content Brief]

[7]. Yang LP, et al. Spotlight on histamine dihydrochloride in acute myeloid leukaemia. Drugs Aging. 2011 Apr 1;28(4):325-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Histamine dihydrochloride

21 Cited Publications

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Histamine dihydrochloride

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