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Purity: ≥98%
Rasagiline mesylate (TVP-101; TV-1030, TVP-1022; Agn-1135; Azilect) is a potent, selective and irreversible MAO-B (monoamine oxidase B) inhibitor with the potential for the treatment of idiopathic PD/Parkinson's disease. It displays anti-Parkinsonian activity, and exhibits neuroprotective as well as antiapoptotic activity against several neurotoxins in cell culture. Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro.
| ln Vitro |
Following treatment with Dexamethasone (10 µM), the proliferation rates of SH-SY5Y and 1242-MG are dramatically increased by rasagine (0.25 nM; 96 hours)[2].
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| ln Vivo |
In a transgenic model of multiple system atrophy, rasagiline has neuroprotective effects. Motor impairments related to 2.5 mg/kg Rasagiline therapy improve according to motor behavioral tests[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: Neuroblastoma SH-SY5Y, and glioblastoma 1242- MG Tested Concentrations: 0.25 nM Incubation Duration: 96 hrs (hours) Experimental Results: Caused ~60% increase in the cell proliferation rate for SH-SY5Y cells treated with Dexamethasone. Caused ~35% increase in cell proliferation rate for 1242-MG cells treated with Dexamethasone. |
| Animal Protocol |
Animal/Disease Models: (PLP)-α-synuclein transgenic mice over 6 months of age[3]
Doses: Low-(0.8 mg/kg bw) and high dose (2.5 mg/kg bw) Route of Administration: Administered subcutaneously (sc) every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment). Experimental Results: Low dose treatment did not show protective efficacy in striatum with number of neurons similar to placebo treated MSA mice. High dose was associated with about 15% rescue of DARPP-32 immunoreactive striatal neurons. Low dose treatment had no effect on nigral neuronal loss, but high dose completely protected nigral neurons with numbers comparable to healthy controls. |
| References |
[1]. M B Youdim, et al. Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B. Br J Pharmacol. 2001 Jan;132(2):500-6.
[2]. Shawna Tazik, et al. Comparative neuroprotective effects of Rasagiline and aminoindan with selegiline on dexamethasone-induced brain cell apoptosis. Neurotox Res. 2009 Apr;15(3):284-90. [3]. Nadia Stefanova, et al. Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Exp Neurol. 2008 Apr;210(2):421-7. |
| Molecular Formula |
C12H13N.CH4O3S
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| Molecular Weight |
267.34
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| CAS # |
161735-79-1
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| Related CAS # |
Rasagiline;136236-51-6;Rasagiline-13C3 mesylate;1391052-18-8;Rasagiline-13C3 mesylate racemic;1216757-55-9
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| SMILES |
CS(=O)(O)=O.C#CCN[C@H]1C2=CC=CC=C2CC1
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (374.06 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
Solubility in Formulation 2: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7406 mL | 18.7028 mL | 37.4056 mL | |
| 5 mM | 0.7481 mL | 3.7406 mL | 7.4811 mL | |
| 10 mM | 0.3741 mL | 1.8703 mL | 3.7406 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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