Rasagiline (Synonyms: (R)-AGN1135; TVP1012)

Name: Rasagiline
Brand: MedChemExpress
SKU: HY-14605A
Rating: 5.0 (7 reviews)

Cat. No.: HY-14605A Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

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

Rasagiline Chemical Structure

CAS No. : 136236-51-6

Size	Price	Stock	Quantity
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 110	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 110	In-stock	Estimated Time of Arrival: December 31
Solid or liquid
50 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 130	In-stock	Estimated Time of Arrival: December 31
250 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Rasagiline:

(S)-Rasagiline In-stock
Rasagiline mesylate In-stock
Rasagiline-¹³C₃ mesylate racemic Get quote
Rasagiline (Standard) Get quote

6 Publications Citing Use of MCE Rasagiline

: 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.

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MAO-A MAO-B

Biological Activity
Purity & Documentation
References
Customer Review

Description

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^[1]. 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.

IC₅₀ & Target^[1]

rMAO-B

4.43 nM (IC₅₀)

rMAO-A

412 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
BTI-TN-5B1-4	IC₅₀	0.069 μM Compound: Rasagiline	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	[PMID: 23474901]
BTI-TN-5B1-4	IC₅₀	13 nM Compound: Rasagiline	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]
BTI-TN-5B1-4	IC₅₀	13 nM Compound: Rasagiline	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	[PMID: 30522087]
BTI-TN-5B1-4	IC₅₀	147.3 μM Compound: Rasagiline	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	16.44 μM Compound: Rasagiline	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	[PMID: 23474901]
BTI-TN-5B1-4	IC₅₀	3.65 μM Compound: Rasagiline	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	[PMID: 31711793]
BTI-TN-5B1-4	IC₅₀	49.66 nM Compound: Rasagline	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	52974 nM Compound: Rasagline	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	[PMID: 27244485]
BTI-TN-5B1-4	IC₅₀	680 nM Compound: Rasagiline	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	680 nM Compound: Rasagiline	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]
SH-SY5Y	IC₅₀	2700 μM Compound: Rasagiline	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	[PMID: 33360800]
SIM-A9	IC₅₀	2900 μM Compound: Rasagiline	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	[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.

Cell Proliferation Assay^[2]

Cell Line:	Neuroblastoma SH-SY5Y, and glioblastoma 1242-MG
Concentration:	0.25 nM
Incubation Time:	96 hours
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

Rasagiline is neuroprotective in a transgenic model of multiple system atrophy. Motor behavioural tests show improvements in motor deficits associated with 2.5 mg/kg Rasagiline therapy^[3].

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

Animal Model:	(PLP)-α-synuclein transgenic mice over 6 months of age^[3]
Dosage:	Low-(0.8 mg/kg b.w.) and high dose (2.5 mg/kg b. w.)
Administration:	Administered subcutaneously every 24 h for a total period of 4 weeks (from day 1 till day 28 of the experiment).
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.

Clinical Trial

Molecular Weight

171.24

Formula

C₁₂H₁₃N

CAS No.

136236-51-6

Appearance

<38°C Solid,>41°C Liquid

Color

Light yellow to brown

SMILES

C#CCN[C@H]1C2=CC=CC=C2CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (583.97 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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.8397 mL	29.1983 mL	58.3965 mL
5 mM	1.1679 mL	5.8397 mL	11.6793 mL
10 mM	0.5840 mL	2.9198 mL	5.8397 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, 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.

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 (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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (14.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 99.88%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (250 KB) HNMR (217 KB) LCMS (257 KB)

Handling Instructions (2659 KB)

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. [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

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

H₂O / DMSO	1 mM	5.8397 mL	29.1983 mL	58.3965 mL	145.9914 mL
	5 mM	1.1679 mL	5.8397 mL	11.6793 mL	29.1983 mL
	10 mM	0.5840 mL	2.9198 mL	5.8397 mL	14.5991 mL
	15 mM	0.3893 mL	1.9466 mL	3.8931 mL	9.7328 mL
	20 mM	0.2920 mL	1.4599 mL	2.9198 mL	7.2996 mL
	25 mM	0.2336 mL	1.1679 mL	2.3359 mL	5.8397 mL
	30 mM	0.1947 mL	0.9733 mL	1.9466 mL	4.8664 mL
DMSO	40 mM	0.1460 mL	0.7300 mL	1.4599 mL	3.6498 mL
	50 mM	0.1168 mL	0.5840 mL	1.1679 mL	2.9198 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

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.

Keywords:

Rasagiline136236-51-6(R)-AGN1135 TVP1012TVP1012TVP 1012TVP-1012Monoamine OxidaseMAOInhibitorinhibitorinhibit

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Rasagiline (Synonyms: (R)-AGN1135; TVP1012)

Customer Review

Other Forms of Rasagiline:

Rasagiline Related Antibodies

6 Publications Citing Use of MCE Rasagiline

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Monoamine Oxidase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Rasagiline Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

Rasagiline Related Classifications

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