Rasagiline Mesylate

Catalog No.S2102 Synonyms: TVP-1012

For research use only.

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Rasagiline Mesylate Chemical Structure

CAS No. 161735-79-1

Selleck's Rasagiline Mesylate has been cited by 1 Publication

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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.
Targets
MAO-B [1] MAO-A [1]
4.43 nM 412 nM
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]

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 (from reference)

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 267.34
Formula

C12H13N.CH4O3S

CAS No. 161735-79-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04841798 Recruiting Other: [11C]SL25.1188 PET radiotracer Major Depressive Disorder|Treatment Resistant Depression Centre for Addiction and Mental Health April 15 2021 Not Applicable
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 Branded Pharmaceutical Products R&D Inc. March 2010 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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