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Purity: ≥98%
Atipamezole (Antisedan, MPV-1248) is a synthetic α2 adrenergic receptor antagonist with a Ki of 1.6 nM. It has also been studied in humans as a possible medication to treat Parkinson's disease. The aldosterone release was significantly inhibited by atripamezole hydrochloride (range 10-1000 nM). Atipamezole demonstrated an alpha 2/alpha 1 selectivity ratio of 8526 in receptor binding studies involving [3H]-clonidine and [3H]-prazosin displacement. In contrast, idazoxan and yohimbine displayed ratios of 27 and 40, respectively.
| Targets |
α2 adrenergic receptor
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| ln Vivo |
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| Enzyme Assay |
Atipamezole Hcl(MPV1248 Hcl) exhibits high affinity and selectivity for the alpha 2-receptor as an antagonist of alpha-adrenoceptors.
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| Animal Protocol |
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| References |
| Molecular Formula |
C14H16N2.HCL
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| Molecular Weight |
248.75
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| Exact Mass |
248.11
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| Elemental Analysis |
C, 67.60; H, 6.89; Cl, 14.25; N, 11.26
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| CAS # |
104075-48-1
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| Related CAS # |
Atipamezole; 104054-27-5
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| Appearance |
Solid powder
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| SMILES |
CCC1(CC2=CC=CC=C2C1)C3=CN=CN3.Cl
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| InChi Key |
PCCVCJAQMHDWJY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H16N2.ClH/c1-2-14(13-9-15-10-16-13)7-11-5-3-4-6-12(11)8-14;/h3-6,9-10H,2,7-8H2,1H3,(H,15,16);1H
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| Chemical Name |
5-(2-ethyl-1,3-dihydroinden-2-yl)-1H-imidazole;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (10.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (10.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0201 mL | 20.1005 mL | 40.2010 mL | |
| 5 mM | 0.8040 mL | 4.0201 mL | 8.0402 mL | |
| 10 mM | 0.4020 mL | 2.0101 mL | 4.0201 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01435213 | Completed | Drug: Atipamezole Drug: Atomoxetine |
Healthy | University of Turku | September 2011 | Phase 1 |
Products are for research use only; We do not sell to patients
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