Rasagiline Mesylate
For research use only.
Catalog No.S2102 Synonyms: TVP-1012
CAS No. 161735-79-1
Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
Purity & Quality Control
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Biological Activity
| Description | Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease. | ||||
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| Targets |
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| In vitro |
Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro. [1] Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells. [2] Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death. [3] Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase. [4] |
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| In vivo | Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. [1] Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse. [5] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 53 mg/mL (198.24 mM) |
|---|---|---|
| Water | 53 mg/mL (198.24 mM) | |
| Ethanol | 53 mg/mL (198.24 mM) | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): Saline For best results, use promptly after mixing. |
30 mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 267.34 |
|---|---|
| Formula | C12H13N.CH4O3S |
| CAS No. | 161735-79-1 |
| Storage |
powder in solvent |
| Synonyms | TVP-1012 |
| Smiles | CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12 |
In vivo Formulation Calculator (Clear solution)
| Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment) | ||||||||||
| Dosage | mg/kg |  |
Average weight of animals | g | |
Dosing volume per animal | ul | |
Number of animals | |
| Step 2: Enter the in vivo formulation () | ||||||||||
| % DMSO % % Tween 80 % ddH2O | ||||||||||
| CalculateReset | ||||||||||
Calculation results:
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Bio Calculators
Molarity Calculator
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Dilution Calculator
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT01879241 | Completed | Drug: Rasagiline|Drug: Placebo | Amyotrophic Lateral Sclerosis | University of Ulm | June 2013 | Phase 2 |
| NCT01652313 | Completed | Drug: Rasagiline | Parkinson''s Disease | H. Lundbeck A/S | May 2012 | Phase 1 |
| NCT01736891 | Completed | Drug: Rasagiline|Drug: Placebo | Parkinson´s Disease | Chongqing Fortune Pharmaceutical Co. Ltd.|Beijing Bionovo Medicine Development Co. Ltd. | November 2011 | Phase 3 |
| NCT01178047 | Terminated | Drug: Rasagiline | Parkinson''s Disease | University of Zurich|H. Lundbeck A/S | September 2011 | Phase 4 |
| NCT01055379 | Completed | Drug: Rasagiline|Drug: Placebo | Depressive Symptoms|Parkinson''s Disease | Lundbeck Italia S.p.A.|Teva Pharmaceutical Industries | March 2010 | Phase 4 |
| NCT00203164 | Completed | Drug: rasagiline mesylate | Parkinson''s Disease | Teva Pharmaceutical Industries | May 2002 | Phase 3 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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