4-Methylhistamine dihydrochloride
Based on 1 Customer Validation
4-Methylhistamine hydrochloride is the dihydrochloride salt of 4-Methylhistamine (HY-W580721). 4-Methylhistamine hydrochloride is a potent and selective agonist of histamine 4 receptor (H4R) with a Ki of 50 nM. 4-Methylhistamine hydrochloride has a >100-fold selectivity for the hH4R over the other histamine receptor subtypes. 4-Methylhistamine hydrochloride can potently activate the hH4R (pEC50 = 7.4). 4-Methylhistamine hydrochloride can be used for the researches of cancer, inflammation and immunology, such as lung cancer and skin inflammation.
For research use only. We do not sell to patients.
- Purity: 99.35%
- CAS No.: 36376-47-3
- Formula: C6H13Cl2N3
- Molecular Weight:198.10
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, 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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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H4 receptor |
4-Methylhistamine (1-10 μM, 12 h) hydrochloride inhibits cell proliferation in A549, H157, H460 and H322 cells[4].
4-Methylhistamine (1 μM, 12 h) hydrochloride 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) hydrochloride 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) hydrochloride decreases the average tumour volume and prolongs survival in A549 tumor mice[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:Increase 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[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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CAS No. 36376-47-3
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Appearance Solid
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Molecular Weight 198.10
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Formula C6H13Cl2N3
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Color Off-white to light brown
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SMILES
[H]Cl.CC1=C(CCN)NC=N1.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H2O : 125 mg/mL (630.99 mM; Need ultrasonic)
DMSO : 20 mg/mL (100.96 mM; Need ultrasonic and warming; 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 (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.
* 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 (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.
* 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)
Purity & Documentation
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Data Sheet (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[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]
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 (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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.0480 mL | 25.2398 mL | 50.4796 mL | 126.1989 mL |
| 5 mM | 1.0096 mL | 5.0480 mL | 10.0959 mL | 25.2398 mL | |
| 10 mM | 0.5048 mL | 2.5240 mL | 5.0480 mL | 12.6199 mL | |
| 15 mM | 0.3365 mL | 1.6827 mL | 3.3653 mL | 8.4133 mL | |
| 20 mM | 0.2524 mL | 1.2620 mL | 2.5240 mL | 6.3099 mL | |
| 25 mM | 0.2019 mL | 1.0096 mL | 2.0192 mL | 5.0480 mL | |
| 30 mM | 0.1683 mL | 0.8413 mL | 1.6827 mL | 4.2066 mL | |
| 40 mM | 0.1262 mL | 0.6310 mL | 1.2620 mL | 3.1550 mL | |
| 50 mM | 0.1010 mL | 0.5048 mL | 1.0096 mL | 2.5240 mL | |
| 60 mM | 0.0841 mL | 0.4207 mL | 0.8413 mL | 2.1033 mL | |
| 80 mM | 0.0631 mL | 0.3155 mL | 0.6310 mL | 1.5775 mL | |
| 100 mM | 0.0505 mL | 0.2524 mL | 0.5048 mL | 1.2620 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.
4-Methylhistamine dihydrochloride Related Classifications
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