Safinamide (Synonyms: FCE 26743; EMD 1195686)

Name: Safinamide
Brand: MedChemExpress
SKU: HY-70057
Rating: 5.0 (2 reviews)

Cat. No.: HY-70057 Purity: 99.89%: FAQs
Data Sheet SDS COA Handling Instructions

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Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM). Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al.

For research use only. We do not sell to patients.

Safinamide Chemical Structure

CAS No. : 133865-89-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 44	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 44	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 59	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 101	In-stock	Estimated Time of Arrival: December 31
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Based on 2 publication(s) in Google Scholar

Other Forms of Safinamide:

(R)-Safinamide Get quote
Safinamide-d4 Get quote
Safinamide-d₄-1 Get quote
Safinamide mesylate Get quote
Safinamide (Standard) Get quote

2 Publications Citing Use of MCE Safinamide

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MAO-A MAO-B

Biological Activity
Purity & Documentation
References
Customer Review

Description

Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC₅₀=0.098 µM) over MAO-A (IC₅₀=580 µM)^[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC₅₀=8 µM) than at resting (IC₅₀=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al^[2]^[3].

IC₅₀ & Target^[1]

MAO-B

98 nM (IC₅₀)

MAO-A

580 μM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	> 25900 nM Compound: SAF	Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method	[PMID: 31265934]
BTI-TN-5B1-4	IC₅₀	0.0231 μM Compound: Safinamide	Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho	[PMID: 31711793]
BTI-TN-5B1-4	IC₅₀	23.07 nM Compound: Safinamide	Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay Inhibition of human microsomal MAO-B expressed in recombinant baculovirus infected insect BTI-TN-5B1-4 cells assessed as reduction in H2O2 production using p-tyramine as substrate after 15 mins by fluorescence assay	[PMID: 27244485]
BTI-TN-5B1-4	IC₅₀	25900 nM Compound: SAF	Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay Inhibition of human recombinant MAO-A expressed in baculovirus infected BTI-TN-5B1-4 insect cells using p-tyramine as substrate preincubated for 15 mins and measured after 45 mins by resorufin-based fluorescence assay	[PMID: 30522087]
BTI-TN-5B1-4	IC₅₀	5.18 nM Compound: SAF	Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method Inhibition of human recombinant MAO-B expressed in baculovirus infected BTI-TN-5B1-4 insect cells assessed as decrease in H2O2 production using p-tyramine as substrate incubated for 20 mins by horse-radish peroxidase/amplex red-based fluorescence method	[PMID: 31265934]

In Vitro

Safinamide (1–300 µM) reduces the amplitude of the peak sodium currents in a concentration-dependent manner. When currents are stimulated to a V_test of +10 mV from a V_h of -110 mV, the IC₅₀ value was 262 µM. When the holding potential is depolarized to -53 mV, the inhibitory effect of safinamide with a lower IC₅₀ value (8 µM) in rat cortical neurons^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Safinamide (intraperitoneal injection; 90 mg/kg; once daily; 14 days) treatment prior to MCAO significantly ameliorates MCAO-caused cerebral infarction volume, neurological deficit, disruption of the brain-blood barrier (BBB), and impairs expression of tight junction protein occludin and ZO-1 in mice^[3].
Safinamide (intraperitoneal injection; 5 mg/kg, 15 mg/kg and 30 mg/kg) dose dependently inhibits the veratridine-induced GABA release and Glu release in vivo. At the dose 30 mg/kg, Safinamide prevents the effect of veratridine both on Glu (treatment F1,8=1.31; time×treatment interaction F8,64=2.4) and GABA (treatment F1,8=4.04; time F8,64=3.76, time×treatment interaction F8,64 = 2.83) release.
Safinamide causes a slight, albeit not significant, reduction of veratridine-stimulated Glu release at 0.5 mg/kg and full inhibition at 5 and 15 mg/kg in rat^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Focal cerebral ischemia C57/BL6 male mouse Model^[3]
Dosage:	90 mg/kg
Administration:	Intraperitoneal injection; once daily; 14 days
Result:	Significantly decreased infarction volume in brain areas.

Clinical Trial

Molecular Weight

302.34

Formula

C₁₇H₁₉FN₂O₂

CAS No.

133865-89-1

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H](NCC1=CC=C(OCC2=CC(F)=CC=C2)C=C1)C)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (330.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.3075 mL	16.5377 mL	33.0753 mL
5 mM	0.6615 mL	3.3075 mL	6.6151 mL
10 mM	0.3308 mL	1.6538 mL	3.3075 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.27 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.27 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.89%

Select Batch:

Data Sheet (273 KB) SDS (392 KB)

COA (243 KB) RP-HPLC (177 KB)

Handling Instructions (2659 KB)

References

[1]. Leonetti F, et al. Solid-phase synthesis and insights into structure-activity relationships of safinamide analogues as potent and selective inhibitors of type B monoamine oxidase. J Med Chem, 2007, 50(20), 4909-4916. [Content Brief]

[2]. C Caccia, et al.Safinamide: from molecular targets to a new anti-Parkinson drug. Neurology. 2006 Oct 10;67(7 Suppl 2):S18-23. [Content Brief]

[3]. Michele Morari, et al. Safinamide Differentially Modulates In Vivo Glutamate and GABA Release in the Rat Hippocampus and Basal Ganglia.J Pharmacol Exp Ther. 2018 Feb;364(2):198-206. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.3075 mL	16.5377 mL	33.0753 mL	82.6884 mL
	5 mM	0.6615 mL	3.3075 mL	6.6151 mL	16.5377 mL
	10 mM	0.3308 mL	1.6538 mL	3.3075 mL	8.2688 mL
	15 mM	0.2205 mL	1.1025 mL	2.2050 mL	5.5126 mL
	20 mM	0.1654 mL	0.8269 mL	1.6538 mL	4.1344 mL
	25 mM	0.1323 mL	0.6615 mL	1.3230 mL	3.3075 mL
	30 mM	0.1103 mL	0.5513 mL	1.1025 mL	2.7563 mL
	40 mM	0.0827 mL	0.4134 mL	0.8269 mL	2.0672 mL
	50 mM	0.0662 mL	0.3308 mL	0.6615 mL	1.6538 mL
	60 mM	0.0551 mL	0.2756 mL	0.5513 mL	1.3781 mL
	80 mM	0.0413 mL	0.2067 mL	0.4134 mL	1.0336 mL
	100 mM	0.0331 mL	0.1654 mL	0.3308 mL	0.8269 mL

Safinamide Related Classifications

Neurological Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Safinamide (Synonyms: FCE 26743; EMD 1195686)

Customer Review

Other Forms of Safinamide:

Safinamide Related Antibodies

2 Publications Citing Use of MCE Safinamide

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Monoamine Oxidase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Safinamide Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Safinamide Related Classifications

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