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Rasagiline Mesylate

Name: Rasagiline Mesylate
Brand: Selleck Chemicals
SKU: S2102
Rating: 5 (3 reviews)

Synonyms: TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate

Catalog No.S2102 Purity:99.85%

Rasagiline Mesylate (TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Rasagiline Mesylate Chemical Structure

CAS No. 161735-79-1

Purity & Quality Control

Batch: S210201 DMSO]53 mg/mL]false]Water]53 mg/mL]false]Ethanol]53 mg/mL]false Purity: 99.85%

99.85

Rasagiline Mesylate Related Products

Related Targets	MAO-A MAO-B	Click to Expand
Related Products	Moclobemide (Ro 111163) Sennoside A Paeonol J147 Isatin	Click to Expand
Related Compound Libraries	Metabolism Compound Library Anti-cancer Metabolism Compound Library Glutamine Metabolism Compound Library Carbohydrate Metabolism Compound Library Lipid Metabolism Compound Library	Click to Expand

Signaling Pathway

MAO Signaling Pathway

Biological Activity

Description

Rasagiline Mesylate (TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Targets

MAO-B ^[1]	MAO-A ^[1]
4.43 nM	412 nM

In vitro
In vitro	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. ^[1] Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells. ^[2] Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death. ^[3] Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase. ^[4]

In Vivo
In vivo	Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. ^[1] Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04841798	Completed	Major Depressive Disorder\|Treatment Resistant Depression	Centre for Addiction and Mental Health	April 15 2021	Not Applicable
NCT01879241	Completed	Amyotrophic Lateral Sclerosis	University of Ulm	June 2013	Phase 2
NCT01652313	Completed	Parkinson''s Disease	H. Lundbeck A/S	May 2012	Phase 1
NCT01736891	Completed	Parkinson´s Disease	Chongqing Fortune Pharmaceutical Co. Ltd.\|Beijing Bionovo Medicine Development Co. Ltd.	November 2011	Phase 3
NCT01178047	Terminated	Parkinson''s Disease	University of Zurich\|H. Lundbeck A/S	September 2011	Phase 4
NCT01055379	Completed	Depressive Symptoms\|Parkinson''s Disease	Lundbeck Italia S.p.A.\|Teva Branded Pharmaceutical Products R&D Inc.	March 2010	Phase 4

References

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Chemical Information & Solubility

Molecular Weight	267.34	Formula	C₁₂H₁₃N.CH₄O₃S
CAS No.	161735-79-1	SDF	Download Rasagiline Mesylate SDF
Smiles	CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 53 mg/mL ( (198.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 53 mg/mL

Ethanol : 53 mg/mL

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Clear solution	saline	53.000mg/ml (198.25mM)	Taking the 1 mL working solution as an example, add 53 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (112.22mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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