Histamine (Synonyms: Ergamine)

Name: Histamine
Brand: MedChemExpress
SKU: HY-B1204
Rating: 5.0 (11 reviews)

Cat. No.: HY-B1204 Purity: 99.99%: Data Sheet
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Histamine is the agonist for histamine receptor and a vasodilator. Histamine is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine 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 Chemical Structure

CAS No. : 51-45-6

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
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100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Histamine:

Histamine-α,α,β,β-d₄ dihydrochloride In-stock
Histamine phosphate In-stock
Histamine dihydrochloride In-stock
Histamine (Standard) In-stock
Histamine-d₄ Get quote

11 Publications Citing Use of MCE Histamine

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View All Akt Isoform Specific Products:

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Akt Akt1 Akt2 Akt3

View All p38 MAPK Isoform Specific Products:

View All Isoforms

p38 MAPK p38α p38β MAPK13 p38δ p38γ

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Human Endogenous Metabolite

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	640 nM Compound: Histamine	Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting	[PMID: 20384344]
HEK293	EC₅₀	13 nM Compound: Histamine	Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay Agonist activity at human SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay	[PMID: 27007611]
HEK293	EC₅₀	94 nM Compound: Histamine	Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay Agonist activity at mouse SF-His6-tagged histamine H4 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated response incubated for 5 hrs by luciferase reporter gene assay	[PMID: 27007611]
Sf9	EC₅₀	11 nM Compound: Histamine	Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay Agonist activity at human histamine H4 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay	[PMID: 27007611]
Sf9	EC₅₀	11.6 nM Compound: 1	Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay Activity at human recombinant histamine H4 receptor-RGS4 fusion protein expressed in Sf9 cells coexpressing Galphai2 and G-beta-1-gamma-2 by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	1200 nM Compound: 1	Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay Activity at human recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	1200 nM Compound: 1	Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay Activity at guinea pig recombinant histamine H2 receptor-Gsalpha fusion protein expressed in Sf9 cells by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	13 nM Compound: Histamine	Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay	[PMID: 27007611]
Sf9	EC₅₀	190 nM Compound: Histamine	Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP Agonist activity at human histamine H1 receptor expressed in sf9 cell membrane co-expressing RGS4 or RGS9 assessed as increase in 32Pi level incubated for 20 mins by liquid scintillation counting in presence of [gamma32P]GTP	[PMID: 27007611]
Sf9	EC₅₀	190 nM Compound: 1	Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay Activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 by steady-state GTPase activity assay	[PMID: 18950149]
Sf9	EC₅₀	25.1 nM Compound: 1	Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay	[PMID: 18950149]

In Vitro

Histamine (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 (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 (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:	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.

Clinical Trial

Molecular Weight

111.15

Formula

C₅H₉N₃

CAS No.

51-45-6

Appearance

Solid

Color

White to yellow

SMILES

NCCC1=CN=CN1

Structure Classification

Others

Initial Source

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen, away from moisture

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

Solvent & Solubility

In Vitro:

H₂O : 125 mg/mL (1124.61 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	8.9969 mL	44.9843 mL	89.9685 mL
5 mM	1.7994 mL	8.9969 mL	17.9937 mL
10 mM	0.8997 mL	4.4984 mL	8.9969 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 (stored under nitrogen, 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.

* 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 (899.69 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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

Purity: 99.99%

Select Batch:

Data Sheet (284 KB) SDS (645 KB)

COA (245 KB) HNMR (226 KB) RP-HPLC (241 KB) MS (176 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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	8.9969 mL	44.9843 mL	89.9685 mL	224.9213 mL
	5 mM	1.7994 mL	8.9969 mL	17.9937 mL	44.9843 mL
	10 mM	0.8997 mL	4.4984 mL	8.9969 mL	22.4921 mL
	15 mM	0.5998 mL	2.9990 mL	5.9979 mL	14.9948 mL
	20 mM	0.4498 mL	2.2492 mL	4.4984 mL	11.2461 mL
	25 mM	0.3599 mL	1.7994 mL	3.5987 mL	8.9969 mL
	30 mM	0.2999 mL	1.4995 mL	2.9990 mL	7.4974 mL
	40 mM	0.2249 mL	1.1246 mL	2.2492 mL	5.6230 mL
	50 mM	0.1799 mL	0.8997 mL	1.7994 mL	4.4984 mL
	60 mM	0.1499 mL	0.7497 mL	1.4995 mL	3.7487 mL
	80 mM	0.1125 mL	0.5623 mL	1.1246 mL	2.8115 mL
	100 mM	0.0900 mL	0.4498 mL	0.8997 mL	2.2492 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.

Histamine Related Classifications

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.

Keywords:

Histamine51-45-6ErgamineAktp38 MAPKReactive Oxygen Species (ROS)Histamine ReceptorEndogenous MetaboliteApoptosisPKBProtein kinase Borganic nitrogenimmune responsesintestinal physiological functionsneurotransmitterInhibitorinhibitorinhibit

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Histamine (Synonyms: Ergamine)

Customer Review

Other Forms of Histamine:

Histamine Related Antibodies

11 Publications Citing Use of MCE Histamine

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Akt Isoform Specific Products:

View All p38 MAPK Isoform Specific Products:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Histamine Related Antibodies

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Complete Stock Solution Preparation Table

Histamine Related Classifications

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