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Rasagiline mesylate
Rasagiline mesylate
ChemFaces products have been cited in many studies from excellent and top scientific journals
Product Name Rasagiline mesylate
Price: $70 / 20mg
CAS No.: 161735-79-1
Catalog No.: CFN90004
Molecular Formula: C13H17NO3S
Molecular Weight: 267.34 g/mol
Purity: >=98%
Type of Compound: Alkaloids
Physical Desc.: Powder
Source:
Solvent: DMSO, Pyridine, Methanol, Ethanol, etc.
Download: COA    MSDS    SDF
Similar structural: Comparison (Web)  (SDF)
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Size /Price /Stock 10 mM * 1 mL in DMSO / $20.7 / In-stock
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Related Screening Libraries
Size /Price /Stock 10 mM * 100 uL in DMSO / Inquiry / In-stock
10 mM * 1 mL in DMSO / Inquiry / In-stock
Related Libraries
Biological Activity
Description: Rasagiline mesylate is a potent, selective, non-reversible MAO-B inhibitor, with neuroprotective activities, with anti-Parkinson activity. Rasagiline mesylate exhibits neuroprotective and anti-apoptotic activity against several neurotoxins in cell culture.
Targets: MAO | ROS
In vitro:
Int J Pharm Investig. 2015 Apr-Jun;5(2):87-91.
Effect of the moist-heat sterilization on fabricated nanoscale solid lipid particles containing rasagiline mesylate.[Pubmed: 25838993 ]
Nanoscale solid lipid particles of Rasagiline mesylate (RM) were fabricated by microemulsion technique. The nanoscale particle must be sterile for intravenous administration, and several approaches are available for sterilization. However, the selection of sterilization technique for the fabricated RM loaded nanoscale solid lipid particles mainly depends on the nature of the drug that needs to be encapsulated and release pattern of the polymer.
METHODS AND RESULTS:
We have preferred moist heat sterilization, as it is the most convenient and the composition of the carrier and incorporated drug should remain unchanged and the incorporated drug should not leak out of the drug carrier. The physical and chemical stability of RM loaded nanoscale solid lipid particles investigated during sterilization and to determine the average mean particle size, polydispersity index, zeta potential (ZP), transmission electron microscopy (TEM), entrapment efficiency (EE), and drug content after autoclaving. There were no significant changes in the average mean particle size, polydispersity index, ZP, TEM, EE, and drug content of RM loaded nanoscale solid lipid particles after autoclaving (121°C for 20 min [15 lbs]).
CONCLUSIONS:
These observations suggest that the moist heat sterilization by autoclaving is the most suitable method for nanoscale solid lipid formulations.
Int J Pharm. 2012 Nov 15;438(1-2):266-78.
Controlled release of rasagiline mesylate promotes neuroprotection in a rotenone-induced advanced model of Parkinson's disease.[Pubmed: 22985602]
Microencapsulation of Rasagiline mesylate (RM) into PLGA microspheres was performed by method A (O/W emulsion) and method B (W/O/W double emulsion). The best formulation regarding process yield, encapsulation efficiency and in vitro drug release was that prepared with method A, which exhibited constant drug release for two weeks (K(0)=62.3 μg/day/20mg microspheres).
METHODS AND RESULTS:
Exposure of SKN-AS cells to peroxide-induced oxidative stress (1 mM) resulted in cell apoptosis which was significantly reduced by RM (40.7-102.5 μM) as determined by cell viability, ROS production and DNA fragmentation. Daily doses of rotenone (2 mg/kg) given i.p. to rats for 45 days induced neuronal and behavioral changes similar to those occurring in PD. Once an advanced stage of PD was achieved, animals received RM in saline (1 mg/kg/day) or encapsulated within PLGA microspheres (amount of microspheres equivalent to 15 mg/kg RM given on days 15 and 30). After 45 days RM showed a robust effect on all analytical outcomes evaluated with non-statistically significant differences found between its administration in solution or within microparticles however; with this controlled release system administration of RM could be performed every two weeks thereby making this new therapeutic system an interesting approach for the treatment of PD.
In vivo:
Clin Neuropharmacol. 2000 Nov-Dec;23(6):324-30.
Rasagiline mesylate, a new MAO-B inhibitor for the treatment of Parkinson's disease: a double-blind study as adjunctive therapy to levodopa.[Pubmed: 11575866]
Rasagiline mesylate (TVP-1012) is a potent, selective, non-reversible MAO-B inhibitor, without the tyramine-potentiating effect and with neuroprotective activities. The benefit of rasagiline as monotherapy in patients with early Parkinson's disease (PD) has already been reported.
METHODS AND RESULTS:
To evaluate the safety, tolerability, and clinical effect of rasagiline as adjunctive therapy to levodopa, a multicenter, double-blind, randomized, placebo-controlled, parallel-group study (0.5, 1, and 2 mg/d) was conducted for 12 weeks in 70 patients with PD (mean age, 57.4 y; mean disease duration, 5.7 y; 32 patients had motor fluctuations). A beneficial clinical effect was observed in fluctuating patients treated with rasagiline (all doses), expressed as a decrease in total Unified Parkinson's Disease Rating Scale (UPDRS) score (23.0% vs 8.5% in the placebo group). The treatment effect was still evident 6 weeks after drug discontinuation (in all doses). The safety and tolerability of rasagiline were good. Adverse events were no different than those of patients taking placebo. Almost complete platelet MAO-B inhibition was obtained at all rasagiline doses.
CONCLUSIONS:
This study has demonstrated that rasagiline (up to 2 mg/day) has a good safety profile and a beneficial clinical effect in fluctuating patients with PD when given as an add-on to chronic levodopa therapy.
Rasagiline mesylate Description
Source:
Solvent: DMSO, Pyridine, Methanol, Ethanol, etc.
Storage: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months(2-8C).

Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com

After receiving: The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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Recently, ChemFaces products have been cited in many studies from excellent and top scientific journals

Cell. 2018 Jan 11;172(1-2):249-261.e12.
doi: 10.1016/j.cell.2017.12.019.
IF=36.216(2019)

PMID: 29328914

Cell Metab. 2020 Mar 3;31(3):534-548.e5.
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Calculate Dilution Ratios(Only for Reference)
1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.7406 mL 18.7028 mL 37.4056 mL 74.8111 mL 93.5139 mL
5 mM 0.7481 mL 3.7406 mL 7.4811 mL 14.9622 mL 18.7028 mL
10 mM 0.3741 mL 1.8703 mL 3.7406 mL 7.4811 mL 9.3514 mL
50 mM 0.0748 mL 0.3741 mL 0.7481 mL 1.4962 mL 1.8703 mL
100 mM 0.0374 mL 0.187 mL 0.3741 mL 0.7481 mL 0.9351 mL
* Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
Protocol
Structure Identification:
Eur J Pharm Biopharm. 2013 Nov;85(3 Pt B):1075-83.
Evaluation of different substrates for inkjet printing of rasagiline mesylate.[Pubmed: 23563101]
The main goal of the present study was to evaluate applicability of the different model substrates, namely orodispersible films (ODFs), porous copy paper sheets, and water impermeable transparency films (TFs) in preparation of the inkjet-printed drug-delivery systems. Rasagiline mesylate (RM) was used as a low-dose active pharmaceutical ingredient (API).
METHODS AND RESULTS:
Flexible doses of the drug in a single unit were obtained by printing several subsequent layers on top of the already printed ones, using an off-the-shelf consumer thermal inkjet (TIJ) printer. The produced drug-delivery systems were subjected to microscopic and chemical analysis together with solid-state characterization and content uniformity studies. The results revealed that Rasagiline mesylate recrystallized on the surface of ODFs and TFs, and the printed crystals were arranged in lines. No drug crystals were detected after printing on the surface of the copy paper due to absorption of the ink into the matrix of the substrate. The best linear correlation between the dose of the drug and the number of the printing layers was obtained for the porous copy paper. The other two substrates showed poor linearity and unacceptable standard deviations of the printed drug substance due to limited absorption of the API ink into the carrier. The shear stress between the substrate, the print head, and the paper feeding rollers caused smearing of the drug that had been surface-deposited during the earlier printing cycles.
CONCLUSIONS:
In conclusion, this study indicates that the edible substrates with absorption properties similar to copy paper are favorable for successful preparation of drug-delivery systems by TIJ printers.
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