Histamine
Based on 22 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.99%
- CAS No.: 51-45-6
- 화학식: C5H9N3
- 분자량:111.15
-
보관:
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- Protocol
- 순도&문서
- References
-
Help & FAQs
-
HY-101952
Prostaglandin E2Prostaglandin Receptor Agonist -
HY-P0206
BradykininBradykinin Receptor Modulator -
HY-13715
NorepinephrineAdrenergic Receptor Agonist -
HY-B0075
MelatoninMelatonin Receptor Activator -
HY-B0282
Acetylcholine chlorideCholinergic Agonist -
HY-P0201
Substance PNeurotransmitter -
HY-N0832
L-HistidineEndogenous Metabolite -
HY-13433
ThapsigarginER Stress Inducer -
HY-N0067
γ-Aminobutyric acidNeurotransmitter -
HY-B2176
ATPEndogenous Metabolite -
HY-N0390
L-GlutamineEndogenous Metabolite -
HY-B0228
AdenosineEndogenous Autacoid
Publications Citing Use of MedChemExpress (MCE) Histamine
More- Cancer Cell. 2022 Oct 10;40(10):1111-1127.e9. [Abstract]
- Immunity. 2025 Sep 9;58(9):2320-2335.e9. [Abstract]
- Gut Microbes. 2026 Dec 31;18(1):2630475. [Abstract]
- Adv Sci (Weinh). 2023 Mar;10(7):e2203869. [Abstract]
- ACS Sens. 2026 Mar 27;11(3):1891-1907. [Abstract]
- Br J Pharmacol. 2021 Apr;178(7):1669-1683. [Abstract]
- J Agric Food Chem. 2025 Nov 19;73(46):29604-29618. [Abstract]
- mBio. 2022 Oct 26;13(5):e0200422. [Abstract]
- Front Pharmacol. 2019 Nov 15:10:1380. [Abstract]
- Toxics. 2025 Dec 25;14(1):24. [Abstract]
- FASEB J. 2025 Jul 15;39(13):e70778. [Abstract]
- Pharm Res. 2025 Aug;42(8):1315-1329. [Abstract]
- Microbiol Spectr. 2023 Jan 31;11(2):e0469822. [Abstract]
- J Cell Commun Signal. 2023 Mar;17(1):151-165. [Abstract]
- Insect Sci. 2025 Sep 11. [Abstract]
- JID Innov. 2025 Apr 3;5(4):100369. [Abstract]
- Fishes. 2025 Aug 14.
- Biochem Biophys Res Commun. 2025 Apr 1:755:151566. [Abstract]
- Oncol Lett. 2026 Jun 19;32(2):364.
- Biol Pharm Bull. 2023;46(6):864-868. [Abstract]
- bioRxiv. 2026 Mar 30.
- bioRxiv. 2024 June 12.
Customer Validation & Images
-
RT-PCR
-
WB
-
IF
-
IF
-
In Vivo Efficacy Study
All Histamine Receptor Isoforms
MoreAll Endogenous Metabolite Isoforms
More
Biological Activity
제품 설명
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 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 |
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 |
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: 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 |
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 |
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. Further protocols information, click here.
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
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].
(2) The animals are sacrificed 2 hours after histamine injection, and treated with 1% formalin to check for gastric ulcers.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 51-45-6
-
Appearance Solid
-
분자량 111.15
-
화학식 C5H9N3
-
Color White to yellow
-
SMILES
NCCC1=CN=CN1
-
Synonyms
Ergamine
-
Structure Classification
-
Initial Source
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
-20°C, stored under nitrogen, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
Publications (22)
-
Journal Impact Factor
-
Most Recent
-
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 -
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 -
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 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.
-
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
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 -
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 -
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 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.
-
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 -
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 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 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 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).
-
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 -
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 -
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 -
Insect Sci
UV2 and LW opsin genes mediate phototactic responses in the Asian lady beetle, Harmonia axyridis. [Abstract]2025 Sep 11. PMID: 40931758 -
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 -
-
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 -
-
용액&용해도
In Vitro:
H2O : 100 mg/mL (899.69 mM; Need ultrasonic)
DMSO : 50 mg/mL (449.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (899.69 mM); Clear solution; Need ultrasonic
Protocol
-
Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
-
Data Sheet (284 KB)
-
SDS (647 KB)
- English - EN (647 KB)
- Français - FR (647 KB)
- Deutsch - DE (647 KB)
- Norwegian - NO (647 KB)
- Español - ES (647 KB)
- Swedish - SV (647 KB)
- Italian - IT (647 KB)
- Korean - KR (647 KB)
- Portuguese - PT (647 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
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / 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
HY-B1204 Related Classifications
Powered by Bioz