Rasagiline

Catalog No.S5795 Synonyms: TVP-1012

Rasagiline Chemical Structure

Molecular Weight(MW): 171.24

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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Biological Activity

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.
Targets
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].

Protocol

Solubility (25°C)

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.

Chemical Information

Molecular Weight 171.24
Formula

C12H13N

CAS No. 136236-51-6
Storage powder
in solvent
Synonyms TVP-1012

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03727139 Recruiting Parkinson''s Disease Takeda November 1 2018 --
NCT03727139 Recruiting Parkinson''s Disease Takeda November 1 2018 --
NCT03329508 Recruiting Parkinson Disease Pharma Two B Ltd. January 29 2018 Phase 3
NCT03329508 Recruiting Parkinson Disease Pharma Two B Ltd. January 29 2018 Phase 3
NCT02789020 Recruiting Parkinson''s Disease University of Florida|National Institute of Neurological Disorders and Stroke (NINDS) December 2016 Phase 2
NCT02789020 Recruiting Parkinson''s Disease University of Florida|National Institute of Neurological Disorders and Stroke (NINDS) December 2016 Phase 2

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID