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1-Methylhistamine dihydrochloride
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Catalog No. T8790Cas No. 6481-48-7
1-Methylhistamine dihydrochloride is a major metabolite of histamine by histamine N-methyltransferase in the pathway of histidine metabolism. It has been used as a biomarker of histaminergic system activity in the brains of Alzheimer's disease patients as well as those with hypersomnia and other neurological conditions.
1-Methylhistamine dihydrochloride
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Purity: 99.31%
Catalog No. T8790Cas No. 6481-48-7
1-Methylhistamine dihydrochloride is a major metabolite of histamine by histamine N-methyltransferase in the pathway of histidine metabolism. It has been used as a biomarker of histaminergic system activity in the brains of Alzheimer's disease patients as well as those with hypersomnia and other neurological conditions.
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $33 | In Stock | In Stock | |
| 10 mg | $51 | In Stock | In Stock | |
| 25 mg | $97 | In Stock | In Stock | |
| 50 mg | $178 | In Stock | In Stock | |
| 100 mg | $268 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $34 | In Stock | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:99.31%
Appearance:Solid
Color:Black
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Product Introduction
1-Methylhistamine dihydrochloride AI Summary
1-Methylhistamine dihydrochloride is a potent and multi-target inhibitor with a broad range of bioactivities. It inhibits Tyrosyl-DNA Phosphodiesterase (TDP1) with a potency of 7.1 nM, Histone Lysine Methyltransferase G9a with a potency of 22.4 nM, and shows significant inhibitory activity against other targets including JMJD2A-Tudor Domain, Polymerase Iota, Mammalian Selenoprotein Thioredoxin Reductase 1 (TrxR1), and receptors involved in Marburg Virus entry into cells. The compound induces DNA re-replication in MCF 10a normal breast cells (10.3 nM) and SW480 colon adenocarcinoma cells (794.3 nM). Additionally, it is an inhibitor in the antimalarial drug lead development for AMA1-RON. 1-Methylhistamine dihydrochloride exhibits in vivo agonist activity at the histamine H2 receptor in anesthetized rats, stimulating gastric acid secretion relative to histamine, and demonstrates low activity levels at the histamine H1 receptor in guinea pig ileum, inducing a contractile response. Its thin-layer chromatography analysis shows retardation factors (Rf) of 0.56 with the MeOH-NH4OH-H2O solvent system and 0.52 with the EtOCH2CH2OH-HCl(11N)-H2O solvent system..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | 1-Methylhistamine dihydrochloride is a major metabolite of histamine by histamine N-methyltransferase in the pathway of histidine metabolism. It has been used as a biomarker of histaminergic system activity in the brains of Alzheimer's disease patients as well as those with hypersomnia and other neurological conditions. |
| Molecular Weight | 198.09 |
| Formula | C6H13Cl2N3 |
| Cas No. | 6481-48-7 |
| Smiles | Cl.Cl.CN1C=NC(CCN)=C1 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 12 mg/mL (60.58 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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