Home Metabolism MAO inhibitor Safinamide For research use only.

Safinamide

Synonyms: EMD-1195686, PNU-15774E

Safinamide (EMD-1195686, PNU-15774E) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.

Safinamide Chemical Structure

Safinamide Chemical Structure

CAS: 133865-89-1

Purity & Quality Control

Batch: S535701 DMSO] 60 mg/mL] false] ] ] false] ] ] false Purity: 99.98%
99.98

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Biological Activity

Description Safinamide (EMD-1195686, PNU-15774E) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.
Targets
MAO-B [1]
(Microsomal)
16.7 nM(Ki)
In vitro
In vitro The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. Safinamide also blocks sodium and calcium channels[2].
In Vivo
In vivo Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. Safinamide does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. Safinamide is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of safinamide is found excreted in the feces. Safinamide exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days[2].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03887221 Completed Healthy Zambon SpA June 21 2021 Phase 1
NCT03881371 Completed Parkinson Disease Zambon SpA August 1 2019 Phase 3
NCT03968744 Recruiting Idiopathic Parkinson''s Disease (at Later Stage) Alain Kaelin|Clinical Trial Unit Ente Ospedaliero Cantonale|Ente Ospedaliero Cantonale Bellinzona February 18 2019 Phase 4

Chemical lnformation & Solubility

Molecular Weight 302.34 Formula

C17H19FN2O2
CAS No. 133865-89-1 SDF --
Smiles CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 60 mg/mL ( (198.45 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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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