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Catalog No.S5795 Synonyms: TVP-1012

1 publication

Rasagiline Chemical Structure

CAS No. 136236-51-6

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.

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


Solubility (25°C)

In vitro DMSO 34 mg/mL (198.55 mM)
Water 4 mg/mL (23.35 mM)
Ethanol '34 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 171.24


CAS No. 136236-51-6
Storage powder
in solvent
Synonyms TVP-1012
Smiles C#CCNC1CCC2=CC=CC=C12

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04841798 Not yet 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 Pharmaceutical Industries March 2010 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID