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Histamine Histamine Receptor agonist

Name: Histamine
Brand: Selleck Chemicals
SKU: S3968
Availability: InStock
Rating: 5 (2 reviews)

Cat.No.S3968

Histamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist. This compound can be used to induce animal models of Gastric and Intestinal Ulcers.

Chemical Structure

Molecular Weight: 111.15

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Mianserin HCl Ebastine Astemizole Ciproxifan Maleate Rupatadine Lafutidine Cloperastine hydrochloride Mizolastine

Solubility

In vitro
Batch:

DMSO : 22 mg/mL (197.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 22 mg/mL

Ethanol : 22 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.1mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.16mg/ml (1.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	111.15	Formula	C₅H₉N₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	51-45-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Read more about storage stability stock solution CAS number

Mechanism of Action

In vitro	Histamine stimulates the proliferation of human articular chondrocytes in culture. This compound is reported to modify the behaviour of many cell types in vitro, including chondrocytes, fibroblasts, macrophages, epithelial cells, endothelial cells, and T cells. It also modulates the production of many cytokines and the expression of their receptors. This chemical regulates cellular processes through the expression of its receptors. It stimulates the production of matrix metalloproteinases (MMPs)-13 and -3 (collagenase 3 and stromelysin-1, respectively) by histidine decarboxylase (HAC) in vitro.
In vivo	Histamine has a recognised role in allergic and inflammatory reactions and is an important modulator of numerous physiological processes, including cell proliferation, angiogenesis, and vasopermeability. This compound dilates vasculature, increases blood flow, while it induces hyperpermeability in venula. It disrupts endothelial barrier formation of venula indicated by changes in vascular endothelial cadherin (VE-cadherin) localization at endothelial cell junction.
References	[1] https://pubmed.ncbi.nlm.nih.gov/12972479/ [2] https://www.sciencedirect.com/science/article/pii/S1995764510600478 [3] https://pubmed.ncbi.nlm.nih.gov/26158531/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-25)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07785609	NOT_YET_RECRUITING	Advanced Solid Tumors; Malignant Neoplasm	Merck Sharp & Dohme LLC	2026-09-30	PHASE2
NCT07395882	NOT_YET_RECRUITING	Itching	Aalborg University	2026-02-15
NCT06406114	RECRUITING	Drug Allergy; Cephalosporin Allergy; Drug Hypersensitivity; Antibiotic Allergy; Beta Lactam Adverse Reaction; Drug-Induced Anaphylaxis; Cephalosporin Reaction	Massachusetts General Hospital	2025-05-05	PHASE2
NCT07268248	NOT_YET_RECRUITING	Allergic Reaction to Contrast Media; Hypersensitivity Reaction; Computed Tomography; Premedication	Paul Peng, MD PhD MSCR	2026-06
NCT03647072	RECRUITING	Lymphoma	Sherief Abd-Elsalam	2018-08-01	PHASE3
NCT05319730	RECRUITING	Esophageal Squamous Cell Carcinoma	Merck Sharp & Dohme LLC	2023-05-16	PHASE1; PHASE2

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