Amezinium methylsulfate
Based on 1 Customer Validation
Amezinium methylsulfate (Amezinium metilsulfate; Lu-1631) is an orally active indirect-acting sympathomimetic agent, with an IC50 of 5 μM against canine MAO A. Amezinium methylsulfate preferentially inhibits intraneuronal MAO A, blocks norepinephrine reuptake, stimulates α- and β1-adrenergic receptors (α-/β1 AR), and exerts weak α2-adrenergic receptor blocking activity at higher concentrations. Amezinium methylsulfate increases supine and sitting mean blood pressure and plasma norepinephrine levels, accelerates heart rate in some individuals, induces peripheral vasoconstriction, and regulates norepinephrine metabolism. Amezinium methylsulfate can be used for the research of hypotension and related circulatory regulatory disorders.
For research use only. We do not sell to patients.
- Purity : 99.77%
- CAS No.: 30578-37-1
- Formula: C12H15N3O5S
- Molecular Weight:313.33
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
Description
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MAO-A 5 μM (IC50) |
NET |
In Vitro
Amezinium methylsulfate (0.1-1000 μM; 35 min) methylsulfate potently and selectively inhibits MAO A in dog saphenous vein homogenates with an IC50 of 5 μM, while having negligible effect on MAO B (IC50 >1 mM)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 30578-37-1
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Appearance Solid
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Molecular Weight 313.33
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Formula C12H15N3O5S
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Color White to off-white
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SMILES
COC1=CC(N)=CN=[N+]1C2=CC=CC=C2.O=S(OC)([O-])=O
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Synonyms
Amezinium metilsulfate; Lu-1631
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
H2O : 50 mg/mL (159.58 mM; Need ultrasonic)
DMSO : ≥ 34 mg/mL (108.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
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: 11.11 mg/mL (35.46 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (335 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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Handling Instructions (2659 KB)
References
[1]. Kita K, et al. Treatment of neurogenic orthostatic hypotension with amezinium metilsulfate, a new indirect sympathomimetic drug. Neurology. 1988;38(7):1095-1099. [Content Brief]
[2].
Schaps D, et al. Therapeutische Anwendung von Ameziniummetilsulfat--einem neuen, langwirkenden Sympathikomimetikum--bei rückenmarksnaher Leitungsanästhesie. Anasth Intensivther Notfallmed. 1984 Oct;19(5):235-9. German.
[Content Brief]
[3]. Araújo D, et al. On the mechanism of action of amezinium methylsulphate on the dog saphenous vein. Eur J Pharmacol. 1983;90(2-3):203-214. [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 |
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| DMSO / H2O | 1 mM | 3.1915 mL | 15.9576 mL | 31.9152 mL | 79.7881 mL |
| 5 mM | 0.6383 mL | 3.1915 mL | 6.3830 mL | 15.9576 mL | |
| 10 mM | 0.3192 mL | 1.5958 mL | 3.1915 mL | 7.9788 mL | |
| 15 mM | 0.2128 mL | 1.0638 mL | 2.1277 mL | 5.3192 mL | |
| 20 mM | 0.1596 mL | 0.7979 mL | 1.5958 mL | 3.9894 mL | |
| 25 mM | 0.1277 mL | 0.6383 mL | 1.2766 mL | 3.1915 mL | |
| 30 mM | 0.1064 mL | 0.5319 mL | 1.0638 mL | 2.6596 mL | |
| 40 mM | 0.0798 mL | 0.3989 mL | 0.7979 mL | 1.9947 mL | |
| 50 mM | 0.0638 mL | 0.3192 mL | 0.6383 mL | 1.5958 mL | |
| 60 mM | 0.0532 mL | 0.2660 mL | 0.5319 mL | 1.3298 mL | |
| 80 mM | 0.0399 mL | 0.1995 mL | 0.3989 mL | 0.9974 mL | |
| 100 mM | 0.0319 mL | 0.1596 mL | 0.3192 mL | 0.7979 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.
Amezinium methylsulfate Related Classifications
HY-A0275 Related Classifications
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Keywords
- Amezinium
- 30578-37-1
- Amezinium metilsulfate
- Lu-1631
- Lu1631
- Lu 1631
- Lu-1631
- Adrenergic Receptor
- Monoamine Oxidase
- Monoamine Transporter
- Beta Receptor
- MAO
- norepinephrine
- α-receptors
- saphenous vein homogenates
- MAO B
- α2-adrenoceptor
- β1-receptors
- neurogenic orthostatic hypotension
- postural hypotension
- dog
- MAO A
- Inhibitor
- inhibitor
- inhibit