Home Metabolism MAO inhibitor Rasagiline Mesylate

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Rasagiline Mesylate MAO inhibitor

Cat.No.S2102

Rasagiline Mesylate (TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
Rasagiline Mesylate MAO inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 267.34

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Quality Control

Batch: S210201 DMSO]53 mg/mL]false]Water]53 mg/mL]false]Ethanol]53 mg/mL]false Purity: 99.85%
99.85

Chemical Information, Storage & Stability

Molecular Weight 267.34 Formula

C12H13N.CH4O3S

 Storage (From the date of receipt)
CAS No. 161735-79-1 Download SDF Storage of Stock Solutions

Synonyms TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate Smiles CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12

Solubility

In vitro
Batch:

DMSO : 53 mg/mL ( (198.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 53 mg/mL

Ethanol : 53 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Mechanism of Action

Targets/IC50/Ki
MAO-B [1]
4.43 nM
MAO-A [1]
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]
References
  • https://pubmed.ncbi.nlm.nih.gov/16028105/
  • https://pubmed.ncbi.nlm.nih.gov/10082192/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04841798 Completed
Major Depressive Disorder|Treatment Resistant Depression
Centre for Addiction and Mental Health
 April 15 2021 Not Applicable
NCT01879241 Completed
Amyotrophic Lateral Sclerosis
University of Ulm
 June 2013 Phase 2
NCT01652313 Completed
Parkinson''s Disease
H. Lundbeck A/S
 May 2012 Phase 1
NCT01736891 Completed
Parkinson´s Disease
Chongqing Fortune Pharmaceutical Co. Ltd.|Beijing Bionovo Medicine Development Co. Ltd.
 November 2011 Phase 3
NCT01178047 Terminated
Parkinson''s Disease
University of Zurich|H. Lundbeck A/S
 September 2011 Phase 4
NCT01055379 Completed
Depressive Symptoms|Parkinson''s Disease
Lundbeck Italia S.p.A.|Teva Branded Pharmaceutical Products R&D Inc.
 March 2010 Phase 4

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