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Safinamide mesylate

Name: Safinamide mesylate
Brand: TargetMol
SKU: T6651
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T6651Cas No. 202825-46-5

Alias FCE28073 mesylate, EMD 1195686 mesylate

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

Safinamide mesylate

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Purity: 99.67%

Catalog No. T6651Alias FCE28073 mesylate, EMD 1195686 mesylateCas No. 202825-46-5

Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$31	In Stock	In Stock
10 mg	$47	In Stock	In Stock
25 mg	$82	In Stock	In Stock
50 mg	$115	In Stock	In Stock
100 mg	$162	In Stock	In Stock
500 mg	$397	-	In Stock
1 g	$593	-	In Stock
1 mL x 10 mM (in DMSO)	$35	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.67%

Appearance:Solid

Color:White

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COA LCMS HNMR HPLC

Product Introduction

Bioactivity

Description	Safinamide mesylate (EMD 1195686 mesylate) , a mesylate salt of Safinamide, can reversibly and specifically inhibit MAO-B (IC50: 98 nM), has 5918-fold selectivity against MAO-A.
Targets&IC50	MAO-B:98 nM, MAO-A:580 nM
In vitro	Safinamide is a highly specific MAO-B inhibitor in rat brain mitochondria (IC50: 98 nM) and also inhibits MAO-B in human brain (IC50: 9 nM). Safinamide has a high affinity for the Na+ channel-binding site II in rat cortical membranes (IC50: 8 μM). Safinamide concentration- and state-dependently inhibits the fast Na+ currents in rat cortical neurons. Safinamide blocks N-Type Ca2+ currents in rat cortical neurons (IC50: 23 μM). Safinamide inhibits glutamate release induced by depolarizing conditions in rat hippocampal synaptosomes (IC50: 9 μM). Safinamide ( IC50: 1.4 μM) incubated 1 hour before veratridine reduces the neuron damage through blockade of opening voltage-dependent Na+ and Ca2+ channels in rat primary cortical neurons. Safinamide binds to human MAO-B (Ki: 0.5 μM). Safinamide binds to human MAO-B in an extended conformation occupying both flavin and entrance cavity.
In vivo	Safinamide (p.o.) dose-dependently inhibits mouse brain MAO-B (IC50: 0.6 mg/kg), and MAO-B activity recovers quickly, starting from 8 hours. Safinamide markedly inhibits cell body degeneration in the substantia nigra pars compacta. Safinamide intraperitoneally administered 15 minutes before kainic acid protects against hippocampal neuron loss, starting at 10 mg/kg showing neuroprotective properties. Safinamide (100 mg/kg, i.p.) shows a relevant neuro rescuing effect on hippocampal neurons when given 3 hours after ischemia. Safinamide has a high oral bioavailability (80-92%), is rapidly absorbed in plasma after reaching the peak within 0.5-2 hours declines, with a terminal half-life of about 3, 7, and 13 hours in mice, rats, and monkeys, respectively.
Animal Research	Animal Models: DA-depleted C57BL miceFormulation: sterile 0.9% sodium chloride solutionDosages: 20 mg/kgAdministration: Inject intraperitoneally in a single dose
Synonyms	FCE28073 mesylate, EMD 1195686 mesylate

Chemical Properties

Molecular Weight	398.45
Formula	C₁₈H₂₃FN₂O₅S
Cas No.	202825-46-5
Smiles	CS(O)(=O)=O.C[C@H](NCc1ccc(OCc2cccc(F)c2)cc1)C(N)=O
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: 11 mg/mL (27.61 mM), Sonication is recommended.

DMSO: 40 mg/mL (100.39 mM), Sonication is recommended.

H2O: 73 mg/mL (183.21 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.02 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

Ethanol/DMSO/H2O

	1mg	5mg	10mg	50mg
1 mM	2.5097 mL	12.5486 mL	25.0973 mL	125.4863 mL
5 mM	0.5019 mL	2.5097 mL	5.0195 mL	25.0973 mL
10 mM	0.2510 mL	1.2549 mL	2.5097 mL	12.5486 mL
20 mM	0.1255 mL	0.6274 mL	1.2549 mL	6.2743 mL

DMSO/H2O

	1mg	5mg	10mg	50mg
50 mM	0.0502 mL	0.2510 mL	0.5019 mL	2.5097 mL
100 mM	0.0251 mL	0.1255 mL	0.2510 mL	1.2549 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc