Home Metabolism MAO inhibitor Rasagiline For research use only.

Rasagiline

Synonyms: TVP-1012

Rasagiline (TVP-1012) 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 Chemical Structure

Rasagiline Chemical Structure

CAS: 136236-51-6

Selleck's Rasagiline has been cited by 1 publication

Purity & Quality Control

Batch: S579501 DMSO] 34 mg/mL] false] Ethanol] 34 mg/mL] false] Water] 4 mg/mL] false Purity: 99.89%
99.89

Rasagiline Related Products

Signaling Pathway

MAO Signaling Pathways

MAO Signaling Pathway

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Biological Activity

Description Rasagiline (TVP-1012) 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.
Targets
MAO-B [1] MAO-A [1]
4.43 nM 412 nM
In vitro
In vitro 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[2].
In Vivo
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%[1].
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

Chemical Information & Solubility

Molecular Weight 171.24 Formula

C12H13N
CAS No. 136236-51-6 SDF --
Smiles C#CCNC1CCC2=CC=CC=C12
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 34 mg/mL ( (198.55 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 34 mg/mL

Water : 4 mg/mL


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In vivo
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In vivo Formulation Calculator

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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.

Note: 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.

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.

Handling Instructions

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