Safinamide | EMD-1195686 | FCE-26743 | CAS#133865-89-1 | Monoamine Oxidase B Inhibitor

Safinamide
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 326805

CAS#: 133865-89-1 (free base)

Description: Safinamide, also known as FCE-26743 and EMD-1195686, is a drug indicated for the treatment of Parkinson's disease with multiple methods of action. Potential additional uses might be restless legs syndrome (RLS) and epilepsy. Safinamide is a reversible and selective monoamine oxidase B inhibitor, reducing degradation of dopamine, and a glutamate release inhibitor. It also inhibits dopamine reuptake. Additionally, safinamide blocks sodium and calcium channels. Safinamide has been approved by the European Medicines Agency for the treatment of adult patients with idiopathic Parkinson’s disease as add-on therapy to a stable dose of Levodopa (L-dopa) alone or in combination with other PD drugs in patients with mid-to-late-stage fluctuating disease.

Chemical Structure

Safinamide

CAS# 133865-89-1 (free base)

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 326805
Name: Safinamide
CAS#: 133865-89-1 (free base)
Chemical Formula: C17H19FN2O2
Exact Mass: 302.14
Molecular Weight: 302.350
Elemental Analysis: C, 67.53; H, 6.33; F, 6.28; N, 9.27; O, 10.58

Price and Availability

Size	Price	Availability
100mg	USD 90	Ready to ship
200mg	USD 150	Ready to ship
500mg	USD 250	Ready to ship
1g	USD 450	Ready to ship
2g	USD 650	Ready to ship
5g	USD 950	Ready to ship
10g	USD 1450	Ready to ship
100g	USD 3850	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Related CAS #: 133865-89-1 (free base) 202825-46-5 (mesylate)

Synonym: FCE-28073; FCE 28073; FCE28073; NW 1015; NW1015; NW-1015; PNU 151774E; PNU-151774E; EMD-1195686; EMD1195686; EMD 1195686; Safinamide, Xadago

IUPAC/Chemical Name: (S)-2-((4-((3-fluorobenzyl)oxy)benzyl)amino)propanamide

InChi Key: NEMGRZFTLSKBAP-LBPRGKRZSA-N

InChi Code: InChI=1S/C17H19FN2O2/c1-12(17(19)21)20-10-13-5-7-16(8-6-13)22-11-14-3-2-4-15(18)9-14/h2-9,12,20H,10-11H2,1H3,(H2,19,21)/t12-/m0/s1

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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:

Product Data

Certificate of Analysis:

View CoA: current batch, Lot#A9T02K19

QC Data:

View QC data: current batch, Lot#A9T02K19

Safety Data Sheet (SDS):

View Safety Data Sheet (SDS)

Instruction:

View handling instruction

Biological target:	Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM).
In vitro activity:	Safinamide might have potential for the prevention and therapy of Alzheimer's disease. In amyloid (Aβ)1-42 oligomers-stimulated M17 neuronal cells, safinamide ameliorated Aβ1-42 oligomers-induced oxidative stress. Safinamide treatment significantly ameliorated SA-β-gal-positive cells and telomerase activity. Safinamide treatment resulted in decreased mRNA and protein expressions of p21 and plasminogen activator inhibitor-1 (PAI-1). Reference: Bioengineered. 2022 Jan;13(1):1921-1930. https://pubmed.ncbi.nlm.nih.gov/35001806/
In vivo activity:	In a rat model of chronic constriction injury (CCI), safinamide improved neuropathic pain in male CCI rats. Single oral administration of safinamide dose-dependently improved neuropathic pain in pain assessments on day 14. With repeated administration, the effect of safinamide on pain was enhanced. Reference: Behav Brain Res. 2023 Aug 24;452:114555. https://pubmed.ncbi.nlm.nih.gov/37355233/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	60.0	198.45

Preparing Stock Solutions

The following data is based on the product molecular weight 302.35 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Gu X, Zhang G, Qin Z, Yin M, Chen W, Zhang Y, Liu X. Safinamide protects against amyloid β (Aβ)-induced oxidative stress and cellular senescence in M17 neuronal cells. Bioengineered. 2022 Jan;13(1):1921-1930. doi: 10.1080/21655979.2021.2022262. PMID: 35001806; PMCID: PMC8805854. 2. Qian L, Li JZ, Sun X, Chen JB, Dai Y, Huang QX, Jin YJ, Duan QN. Safinamide prevents lipopolysaccharide (LPS)-induced inflammation in macrophages by suppressing TLR4/NF-κB signaling. Int Immunopharmacol. 2021 Jul;96:107712. doi: 10.1016/j.intimp.2021.107712. Epub 2021 May 31. PMID: 34162132. 3. Kogo Y, Koebis M, Kobayashi Y, Ishida T, Maeda T. Analgesic effect of safinamide mesylate in a rat model of neuropathic pain. Behav Brain Res. 2023 Aug 24;452:114555. doi: 10.1016/j.bbr.2023.114555. Epub 2023 Jun 22. PMID: 37355233. 4. Morari M, Brugnoli A, Pisanò CA, Novello S, Caccia C, Melloni E, Padoani G, Vailati S, Sardina M. 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. doi: 10.1124/jpet.117.245100. Epub 2017 Nov 22. PMID: 29167350.
In vitro protocol:	1. Gu X, Zhang G, Qin Z, Yin M, Chen W, Zhang Y, Liu X. Safinamide protects against amyloid β (Aβ)-induced oxidative stress and cellular senescence in M17 neuronal cells. Bioengineered. 2022 Jan;13(1):1921-1930. doi: 10.1080/21655979.2021.2022262. PMID: 35001806; PMCID: PMC8805854. 2. Qian L, Li JZ, Sun X, Chen JB, Dai Y, Huang QX, Jin YJ, Duan QN. Safinamide prevents lipopolysaccharide (LPS)-induced inflammation in macrophages by suppressing TLR4/NF-κB signaling. Int Immunopharmacol. 2021 Jul;96:107712. doi: 10.1016/j.intimp.2021.107712. Epub 2021 May 31. PMID: 34162132.
In vivo protocol:	1. Kogo Y, Koebis M, Kobayashi Y, Ishida T, Maeda T. Analgesic effect of safinamide mesylate in a rat model of neuropathic pain. Behav Brain Res. 2023 Aug 24;452:114555. doi: 10.1016/j.bbr.2023.114555. Epub 2023 Jun 22. PMID: 37355233. 2. Morari M, Brugnoli A, Pisanò CA, Novello S, Caccia C, Melloni E, Padoani G, Vailati S, Sardina M. 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. doi: 10.1124/jpet.117.245100. Epub 2017 Nov 22. PMID: 29167350.

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1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Available from http://www.ncbi.nlm.nih.gov/books/NBK548819/ PubMed PMID: 31644126.

2: Safinamide for Parkinson's disease. Aust Prescr. 2019 Apr;42(2):78-79. doi: 10.18773/austprescr.2019.021. Epub 2018 Feb 28. Review. PubMed PMID: 31048946; PubMed Central PMCID: PMC6478961.

3: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006-. Available from http://www.ncbi.nlm.nih.gov/books/NBK537993/ PubMed PMID: 30835405.

4: Bette S, Shpiner DS, Singer C, Moore H. Safinamide in the management of patients with Parkinson's disease not stabilized on levodopa: a review of the current clinical evidence. Ther Clin Risk Manag. 2018 Sep 18;14:1737-1745. doi: 10.2147/TCRM.S139545. eCollection 2018. Review. PubMed PMID: 30271159; PubMed Central PMCID: PMC6152599.

5: ▼ Safinamide for Parkinson's disease. Drug Ther Bull. 2018 May;56(5):54-57. doi: 10.1136/dtb.2018.5.0623. Review. PubMed PMID: 29760163.

6: Müller T. Safinamide: an add-on treatment for managing Parkinson's disease. Clin Pharmacol. 2018 Apr 5;10:31-41. doi: 10.2147/CPAA.S137740. eCollection 2018. Review. PubMed PMID: 29670409; PubMed Central PMCID: PMC5896660.

7: Teixeira FG, Gago MF, Marques P, Moreira PS, Magalhães R, Sousa N, Salgado AJ. Safinamide: a new hope for Parkinson's disease? Drug Discov Today. 2018 Mar;23(3):736-744. doi: 10.1016/j.drudis.2018.01.033. Epub 2018 Jan 12. Review. PubMed PMID: 29339106.

8: Baker DE, Kim AP. Formulary Drug Review: Safinamide. Hosp Pharm. 2017 Sep;52(8):532-543. doi: 10.1177/0018578717726046. Epub 2017 Aug 18. Review. PubMed PMID: 29276285; PubMed Central PMCID: PMC5735722.

9: Institute for Quality and Efficiency in Health Care. Safinamide: Benefit Assessment According to §35a Social Code Book V [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2015 Aug 13. Available from http://www.ncbi.nlm.nih.gov/books/NBK458393/ PubMed PMID: 29144651.

10: Institute for Quality and Efficiency in Health Care. Safinamide (Addendum to Commission A15-18) [Internet]. Cologne, Germany: Institute for Quality and Efficiency in Health Care (IQWiG); 2015 Nov 5. Available from http://www.ncbi.nlm.nih.gov/books/NBK458416/ PubMed PMID: 29144646.

11: Müller T. Pharmacokinetic drug evaluation of safinamide mesylate for the treatment of mid-to-late stage Parkinson's disease. Expert Opin Drug Metab Toxicol. 2017 Jun;13(6):693-699. doi: 10.1080/17425255.2017.1329418. Review. PubMed PMID: 28537214.

12: deSouza RM, Schapira A. Safinamide for the treatment of Parkinson's disease. Expert Opin Pharmacother. 2017 Jun;18(9):937-943. doi: 10.1080/14656566.2017.1329819. Epub 2017 May 23. Review. PubMed PMID: 28504022.

13: Blair HA, Dhillon S. Safinamide: A Review in Parkinson's Disease. CNS Drugs. 2017 Feb;31(2):169-176. doi: 10.1007/s40263-017-0408-1. Review. PubMed PMID: 28110399.

14: Müller T, Foley P. Clinical Pharmacokinetics and Pharmacodynamics of Safinamide. Clin Pharmacokinet. 2017 Mar;56(3):251-261. doi: 10.1007/s40262-016-0449-5. Review. PubMed PMID: 27665574.

15: Müller T. Emerging approaches in Parkinson's disease - adjunctive role of safinamide. Ther Clin Risk Manag. 2016 Aug 2;12:1151-60. doi: 10.2147/TCRM.S86393. eCollection 2016. Review. PubMed PMID: 27536120; PubMed Central PMCID: PMC4977086.

16: Stocchi F, Torti M. Adjuvant therapies for Parkinson's disease: critical evaluation of safinamide. Drug Des Devel Ther. 2016 Feb 5;10:609-18. doi: 10.2147/DDDT.S77749. eCollection 2016. Review. PubMed PMID: 26917951; PubMed Central PMCID: PMC4751980.

17: Perez-Lloret S, Rascol O. The safety and efficacy of safinamide mesylate for the treatment of Parkinson's disease. Expert Rev Neurother. 2016;16(3):245-58. doi: 10.1586/14737175.2016.1150783. Epub 2016 Feb 19. Review. PubMed PMID: 26849427.

18: Müller T. Safinamide for symptoms of Parkinson's disease. Drugs Today (Barc). 2015 Nov;51(11):653-9. doi: 10.1358/dot.2015.51.11.2414529. Review. PubMed PMID: 26744740.

19: Fabbri M, Rosa MM, Abreu D, Ferreira JJ. Clinical pharmacology review of safinamide for the treatment of Parkinson's disease. Neurodegener Dis Manag. 2015 Dec;5(6):481-96. doi: 10.2217/nmt.15.46. Epub 2015 Nov 20. Review. PubMed PMID: 26587996.

20: Deeks ED. Safinamide: first global approval. Drugs. 2015 Apr;75(6):705-11. doi: 10.1007/s40265-015-0389-7. Review. PubMed PMID: 25851099.

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