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Rasagiline MAO inhibitor

Name: Rasagiline
Brand: Selleck Chemicals
SKU: S5795
Rating: 5 (1 reviews)

Cat.No.S5795

Rasagiline (TVP-1012) is a novel selective and irreversible MAO-B propargylamine inhibitor with in vitro IC50s of 4.43 nM and 412 nM for MAO-B and MAO-A, respectively.

Chemical Structure

Molecular Weight: 171.24

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Quality Control

Batch: S579501 DMSO]34 mg/mL]false]Ethanol]34 mg/mL]false]Water]4 mg/mL]false Purity: 99.89%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.89

Related Targets	Dehydrogenase HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism
Other MAO Inhibitors	Moclobemide (Ro 111163) Sennoside A Paeonol Isatin Hypericin J147 Amezinium (methylsulfate) Xanthoangelol Norharmane Myristicin

Chemical Information, Storage & Stability

Molecular Weight	171.24	Formula	C₁₂H₁₃N	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	136236-51-6	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	TVP-1012			Smiles	C#CCNC1CCC2=CC=CC=C12

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (198.55 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 34 mg/mL

Water : 4 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
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.

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+ %

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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.

Mechanism of Action

Targets/IC₅₀/Ki	MAO-B 4.43 nM MAO-A 412 nM
In vitro	Rasagiline is a highly selective and potent propargylamine inhibitor of monoamine oxidase (MAO) type B. Like other similar propargylamine inhibitors, this compound binds covalently to the N5 nitrogen of the flavin residue of MAO, resulting in irreversible inactivation of the enzyme. It possesses a similar degree of selectivity to selegiline for inhibition of MAO-B as compared with MAO-A, in rat hepatic and brain tissue both in vivo and in vitro. Both inhibitors will inhibit the A form of the enzyme at higher doses.
In vivo	Rasagiline is well absorbed after oral administration and readily crosses the BBB. The oral bioavailability of this compound is 35%, it reaches Tmax after 0.5-1 hours and its half-life is 1.5-3.5 hours. It exerts linear absorption at doses of 1-10 mg/day. This compound undergoes extensive hepatic Metabolism primarily by cytochrome P450 type 1A2 (CYP1A2). Plasma albumin binding is considered to be 60%-70%.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2386362/ [2] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3721659/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
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

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