4-Methylhistamine
4-Methylhistamine is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation.
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- No. CAS: 36507-31-0
- Fòrmula: C6H11N3
- Peso molecular:125.17
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Actividad biológica
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H4 receptor 50 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf9 | EC50 |
12400 nM
Compound: 58
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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
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[PMID: 27007611] |
4-Methylhistamine (1-10 μM, 12 h) inhibits cell proliferation in A549, H157, H460 and H322 cells[4].
4-Methylhistamine (1 μM, 12 h) decreases the TGF-β1 mRNA expression in A549 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, H157, H460 and H322 cells
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Concentration:1 μM
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Incubation Time:12 h
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Result:Increased E-cadherin levels and decreased Vimentin levels.
4-Methylhistamine (20-40 mg/kg, i.p., once a day for 10 days) attenuates Imiquimod (HY-B0180)-induced psoriasis-like skin inflammation in mice[3].
4-Methylhistamine (100 μmol/kg, i.v., every other day for 33 days) decreases the average tumour volume and prolongs survival in A549 tumor mice models[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c mice with chronic restraint[2]
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Dosage:30 mg/kg
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Administration:Intraperitoneally injection, twice a day before 2 days prior to stress
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Result:Increased in the CD4+ T cells as well as in IFN-γ production.
Decreased IL-4 expression.
Upregulated expression of IL-1β, IFN-γ and TNF-α mRNA.
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Animal Model:Imiquimod (HY-B0180)-induced psoriasis-like dermatitis mice[3]
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Dosage:20 and 40 mg/kg
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Administration:Intraperitoneally injection, once a day for 10 days
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Result:Ameliorated the total clinical severity scores.
Attenuated the psoriatic phenotypes, including epidermal hyperplasis, hyperkeratosis and lymphocytes infiltration.
Led to reductions in the levels of Th1 cytokines (TNF-a, IFN-a, and IL-27).
Increased CD4+CD25+FoxP3+ regulatory T (Treg) cells.
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Animal Model:A549 tumor mice models[4]
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Dosage:100 μmol/kg
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Administration:Intravenously injection, every other day for 33 days
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Result:Decreased tumor volume and the proliferation of tumour cells.
Prolonged survival of mice.
Increased the mRNA expression of E-cadherin and decreased Vimentin levels.
Chemical Information
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No. CAS 36507-31-0
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Appearance Solid
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Peso molecular 125.17
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Fòrmula C6H11N3
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Color White to off-white
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SMILES
NCCC1=C(C)N=CN1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Lim HD, et al. Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther. 2005 Sep;314(3):1310-21. [Content Brief]
[2]. Ahmad SF, et al. Stimulation of the histamine 4 receptor with 4-methylhistamine modulates the effects of chronic stress on the Th1/Th2 cytokine balance. Immunobiology. 2015 Mar;220(3):341-9. [Content Brief]
[3]. Kim CH, et al. Inhibitory Effect of Imiquimod-Induced Psoriasis-Like Skin Inflammation in Mice by Histamine H4 Receptor Agonist 4-Methylhistamine. Scand J Immunol. 2016 Jun;83(6):409-17. [Content Brief]
[4]. Cai WK, et al. Activation of histamine H4 receptors decreases epithelial-to-mesenchymal transition progress by inhibiting transforming growth factor-β1 signalling pathway in non-small cell lung cancer. Eur J Cancer. 2014 Apr;50(6):1195-206. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
4-Methylhistamine Related Classifications
HY-W580721 Related Classifications
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