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Safinamide MAO inhibitor

Name: Safinamide
Brand: Selleck Chemicals
SKU: S5357
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S5357

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 this compound for MAO-B is 98 nM.

Chemical Structure

Molecular Weight: 302.34

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

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

99.98

Related Targets	P450 (e.g. CYP17) Dehydrogenase PDE phosphatase PPAR HSP (HSP90) Vitamin Transferase Carbohydrate Metabolism Mitochondrial Metabolism Casein Kinase Serine/threonin kinase Lipoxygenase Phospholipase (e.g. PLA) Retinoid Receptor DPP ACE Peroxidases Fatty Acid Synthase FXR HMG-CoA Reductase Carbonic Anhydrase Lipase Decarboxylase DHFR IDO/TDO Hydroxylase PCSK9 OXPHOS ROR
Related Products	Moclobemide (Ro 111163) Sennoside A Paeonol J147 Isatin

Chemical Information, Storage & Stability

Molecular Weight	302.34	Formula	C₁₇H₁₉FN₂O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	133865-89-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EMD-1195686, PNU-15774E			Smiles	CC(C(=O)N)NCC1=CC=C(C=C1)OCC2=CC(=CC=C2)F

Solubility

In vitro
Batch:

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.000mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC₅₀/Ki	MAO-B ^[1] (Microsomal) 16.7 nM(Ki)
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. This compound also blocks sodium and calcium channels^[2].
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. This compound does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. It 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 this chemical is found excreted in the feces. It 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].
References	https://pubmed.ncbi.nlm.nih.gov/25600407/ https://pubmed.ncbi.nlm.nih.gov/29018297/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03887221	Completed	Healthy	Zambon SpA	June 21 2021	Phase 1
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
NCT01374113	Completed	Renal Impairment	Newron Pharmaceuticals SPA	June 2011	Phase 1

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