Rasagiline
Based on 7 publication(s) in Google Scholar
Rasagiline (R-AGN1135) is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively. Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Pureza : 99.97%
- No. CAS: 136236-51-6
- Fòrmula: C12H13N
- Peso molecular:171.24
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Almacenamiento:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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PEG300Neutral Polymer
Publications Citing Use of MedChemExpress (MCE) Rasagiline
More- J Neuroinflammation. 2025 Apr 29;22(1):125. [Abstract]
- Eur J Med Chem. 2024 Dec 5:279:116842. [Abstract]
- Eur J Med Chem. 2023 Jul 5:255:115417. [Abstract]
- Bioorg Chem. 2023 Sep:138:106654. [Abstract]
- Front Cell Neurosci. 2018 Sep 11:12:309. [Abstract]
- Behav Brain Res. 2024 Feb 29:459:114787. [Abstract]
- Oncotarget. 2018 Jan 30;9(15):12137-12153. [Abstract]
Customer Validation & Images
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
rMAO-B 4.43 nM (IC50) |
rMAO-A 412 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BTI-TN-5B1-4 | IC50 |
0.069 μM
Compound: Rasagiline
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Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
Inhibition of human recombinant microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
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[PMID: 23474901] |
| BTI-TN-5B1-4 | IC50 |
13 nM
Compound: Rasagiline
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Inhibition of human recombinant MAO-B 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-B 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
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[PMID: 30522087] |
| BTI-TN-5B1-4 | IC50 |
13 nM
Compound: Rasagiline
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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
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[PMID: 31265934] |
| BTI-TN-5B1-4 | IC50 |
147.3 μM
Compound: Rasagiline
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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
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[PMID: 31711793] |
| BTI-TN-5B1-4 | IC50 |
16.44 μM
Compound: Rasagiline
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Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
Inhibition of human recombinant microsomal MAO-A expressed in baculovirus infected BTI-TN-5B1-4 cells using p-tyramine as substrate assessed as production of H2O2 incubated for 15 mins followed by substrate addition measured over 15 mins by fluorimetric a
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[PMID: 23474901] |
| BTI-TN-5B1-4 | IC50 |
3.65 μM
Compound: Rasagiline
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Inhibition of human microsomal MAO-A 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-A 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
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[PMID: 31711793] |
| BTI-TN-5B1-4 | IC50 |
49.66 nM
Compound: Rasagline
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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
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[PMID: 27244485] |
| BTI-TN-5B1-4 | IC50 |
52974 nM
Compound: Rasagline
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Inhibition of human microsomal MAO-A 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-A 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
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[PMID: 27244485] |
| BTI-TN-5B1-4 | IC50 |
680 nM
Compound: Rasagiline
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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
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[PMID: 30522087] |
| BTI-TN-5B1-4 | IC50 |
680 nM
Compound: Rasagiline
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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
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[PMID: 31265934] |
| SH-SY5Y | IC50 |
2700 μM
Compound: Rasagiline
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Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells measured after 24 hrs by MTT assay
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[PMID: 33360800] |
| SIM-A9 | IC50 |
2900 μM
Compound: Rasagiline
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Cytotoxicity against mouse SIM-A9 cells measured after 24 hrs by MTT assay
Cytotoxicity against mouse SIM-A9 cells measured after 24 hrs by MTT assay
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[PMID: 33360800] |
In Vitro
Rasagiline (0.25 nM; 96 hours) significantly increases the proliferation rates of SH-SY5Y and 1242-MG upon Dexamethasone (10 μM) treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Neuroblastoma SH-SY5Y, and glioblastoma 1242-MG
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Concentration:0.25 nM
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Incubation Time:96 hours
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Result: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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:(PLP)-α-synuclein transgenic mice over 6 months of age[3]
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Dosage:Low-(0.8 mg/kg b.w.) and high dose (2.5 mg/kg b. w.)
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Administration:Administered subcutaneously every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment).
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Result: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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 136236-51-6
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Appearance <38°C Solid,>41°C Liquid
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Peso molecular 171.24
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Fòrmula C12H13N
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Color Off-white to light yellow
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SMILES
C#CCN[C@H]1C2=CC=CC=C2CC1
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Synonyms
(R)-AGN1135; TVP1012
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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J Neuroinflammation
Repurposing of epalrestat for neuroprotection in parkinson's disease via activation of the KEAP1/Nrf2 pathway. [Abstract]2025 Apr 29;22(1):125. PMID: 40301912 -
Eur J Med Chem
2024 Dec 5:279:116842. PMID: 39260319 -
Eur J Med Chem
Design, synthesis, and SAR study of novel flavone 1,2,4-oxadiazole derivatives with anti-inflammatory activities for the treatment of Parkinson's disease. [Abstract]2023 Jul 5:255:115417. PMID: 37137246 -
Bioorg Chem
Novel flavonoid 1,3,4-oxadiazole derivatives ameliorate MPTP-induced Parkinson's disease via Nrf2/NF-κB signaling pathway. [Abstract]2023 Sep:138:106654. PMID: 37300959 -
Front Cell Neurosci
Differential Regulation of Adhesion and Phagocytosis of Resting and Activated Microglia by Dopamine. [Abstract]2018 Sep 11:12:309. PMID: 30254570 -
Behav Brain Res
Safinamide alleviates hyperalgesia via inhibiting hyperexcitability of DRG neurons in a mouse model of Parkinson's disease. [Abstract]2024 Feb 29:459:114787. PMID: 38042302 -
Oncotarget
Synergistic neuroprotective effect of rasagiline and idebenone against retinal ischemia-reperfusion injury via the Lin28-let-7-Dicer pathway. [Abstract]2018 Jan 30;9(15):12137-12153. PMID: 29552298
Rasagiline purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 30;9(15):12137-12153. [Abstract]
Retinal protection of Rasagiline combined with Idebenone against retinal ischemia-reperfusion (RIR) injury. Western blot analysis for the expression level of brain-derived neurotrophic factor (BDNF) in the whole IR-injured retinas.
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (583.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 5.88 mg/mL (34.34 mM)
* "≥" means soluble, but saturation unknown.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (14.60 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (14.60 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 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
The EdU incorporation assay measures DNA synthesis by adding the thymidine analog 5-ethynyl-2′-deoxyuridine to cells or tissues, where it is incorporated into newly synthesized DNA during S phase. Incorporated EdU is detected by copper-catalyzed azide-alkyne cycloaddition, in which a fluorescent azide covalently reacts with the ethynyl group on EdU, allowing S-phase cells to be detected by fluorescence microscopy, flow cytometry, or high-content imaging. EdU detection does not require DNA denaturation or anti-BrdU antibody access, which preserves sample structure and improves compatibility with immunostaining and multiparameter cytometry compared with BrdU-based detection. EdU can be cytotoxic in a cell-type- and exposure-dependent manner, so pulse duration, concentration, and continuous-labeling designs should be validated for each cell type.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Nadia Stefanova, et al. Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Exp Neurol. 2008 Apr;210(2):421-7. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 5.8398 mL | 29.1988 mL | 58.3976 mL | 145.9939 mL |
| 5 mM | 1.1680 mL | 5.8398 mL | 11.6795 mL | 29.1988 mL | |
| 10 mM | 0.5840 mL | 2.9199 mL | 5.8398 mL | 14.5994 mL | |
| 15 mM | 0.3893 mL | 1.9466 mL | 3.8932 mL | 9.7329 mL | |
| 20 mM | 0.2920 mL | 1.4599 mL | 2.9199 mL | 7.2997 mL | |
| 25 mM | 0.2336 mL | 1.1680 mL | 2.3359 mL | 5.8398 mL | |
| 30 mM | 0.1947 mL | 0.9733 mL | 1.9466 mL | 4.8665 mL | |
| DMSO | 40 mM | 0.1460 mL | 0.7300 mL | 1.4599 mL | 3.6498 mL |
| 50 mM | 0.1168 mL | 0.5840 mL | 1.1680 mL | 2.9199 mL | |
| 60 mM | 0.0973 mL | 0.4866 mL | 0.9733 mL | 2.4332 mL | |
| 80 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8249 mL | |
| 100 mM | 0.0584 mL | 0.2920 mL | 0.5840 mL | 1.4599 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Rasagiline Related Classifications
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