For research use only.
Catalog No.S5795 Synonyms: TVP-1012
CAS No. 136236-51-6
Rasagiline is a novel selective and irreversible MAO-B propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.
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|Description||Rasagiline is a novel selective and irreversible MAO-B propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.|
Rasagiline is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, rasagiline binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. Rasagiline possesses a similar degree of selectivity to selegiline for inhibition of MAO-B as compared with MAO-A, in rat hepatic and brain tissue both in vivo and in vitro. Both inhibitors will inhibit the A form of the enzyme at higher doses.
|In vivo||Rasagiline is well absorbed after oral administration and readily crosses the BBB. The oral bioavailability of rasagiline is 35%, it reaches Tmax after 0.5-1 hours and its half-life is 1.5-3.5 hours. It exerts linear absorption at doses of 1-10 mg/day. Rasagiline undergoes extensive hepatic metabolism primarily by cytochrome P450 type 1A2 (CYP1A2). Plasma albumin binding is considered to be 60%-70%.|
|In vitro||DMSO||34 mg/mL (198.55 mM)|
|Ethanol||34 mg/mL (198.55 mM)|
|Water||4 mg/mL (23.35 mM)|
* 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.
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|
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 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.
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).
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.
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|
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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