Rasagiline | CAS# 136236-51-6 | Monoamine Oxidase Inhibitor

Rasagiline
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 573409

CAS#: 136236-51-6

Description: Rasagiline is a selective and irreversible propargylamine inhibitor of monoamine oxidase type-B (MAO-B) that is not metabolized to amphetamine derivatives. Rasagiline exhibits neuroprotective and antiapoptotic activity against ischemia and several neurotoxins, including SIN-1, MPTP, 6-hydroxydopamine, and N-methyl-(R)-salsolinol.

Chemical Structure

Rasagiline

CAS# 136236-51-6

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 573409
Name: Rasagiline
CAS#: 136236-51-6
Chemical Formula: C12H13N
Exact Mass: 171.10
Molecular Weight: 171.240
Elemental Analysis: C, 84.17; H, 7.65; N, 8.18

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 205
25mg	USD 325
50mg	USD 500
100mg	USD 900
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Azilect, HSDB 7699, Rasagiline, TV 1030, TV-1030

IUPAC/Chemical Name: 1-Indanamine, N-2-propynyl-, (R)-

InChi Key: RUOKEQAAGRXIBM-GFCCVEGCSA-N

InChi Code: 1S/C12H13N/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12/h1,3-6,12-13H,7-9H2/t12-/m1/s1

SMILES Code: C#CCN[C@@H]1CCc2c1cccc2

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO (need ultrasonic)

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

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Product Data:

Product Data

Instruction:

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Biological target:	Rasagiline 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.
In vitro activity:	Compound 6j (a rasagiline-clorgyline hybrid) displayed low toxicity and good neuroprotective effects in SH-SY5Y cell assay. These results indicated that compound 6j was an effective and promising multitarget agent against Alzheimer's disease. Reference: Eur J Med Chem. 2020 Sep 15;202:112475. https://pubmed.ncbi.nlm.nih.gov/32652406/
In vivo activity:	This meta-analysis highlights the superiority of rasagiline/levodopa in improving motor and nonmotor symptoms of Parkinson's disease, with a similar safety profile to that of levodopa in Parkinson's disease with motor fluctuations. Reference: Parkinsons Dis. 2022 Aug 30;2022:4216452. https://pubmed.ncbi.nlm.nih.gov/36081594/

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO (ultrasonic)	100.0	583.98

Preparing Stock Solutions

The following data is based on the product molecular weight 171.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Xie SS, Liu J, Tang C, Pang C, Li Q, Qin Y, Nong X, Zhang Z, Guo J, Cheng M, Tang W, Liang N, Jiang N. Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease. Eur J Med Chem. 2020 Sep 15;202:112475. doi: 10.1016/j.ejmech.2020.112475. Epub 2020 Jun 30. PMID: 32652406. 2. Vale N, Alves C, Sharma V, Lázaro DF, Silva S, Gomes P, Outeiro TF. A new MAP-Rasagiline conjugate reduces α-synuclein inclusion formation in a cell model. Pharmacol Rep. 2020 Apr;72(2):456-464. doi: 10.1007/s43440-019-00032-x. Epub 2020 Jan 15. PMID: 32048262. 3. Kano O, Tsuda H, Hayashi A, Arai M. Rasagiline as Adjunct to Levodopa for Treatment of Parkinson's Disease: A Systematic Review and Meta-Analysis. Parkinsons Dis. 2022 Aug 30;2022:4216452. doi: 10.1155/2022/4216452. PMID: 36081594; PMCID: PMC9448622. 4. Oka H, Sengoku R, Nakahara A, Yamazaki M. Rasagiline does not exacerbate autonomic blood pressure dysregulation in early or mild Parkinson's disease. Clin Park Relat Disord. 2021 Dec 13;6:100124. doi: 10.1016/j.prdoa.2021.100124. PMID: 34977548; PMCID: PMC8689235.
In vitro protocol:	1. Xie SS, Liu J, Tang C, Pang C, Li Q, Qin Y, Nong X, Zhang Z, Guo J, Cheng M, Tang W, Liang N, Jiang N. Design, synthesis and biological evaluation of rasagiline-clorgyline hybrids as novel dual inhibitors of monoamine oxidase-B and amyloid-β aggregation against Alzheimer's disease. Eur J Med Chem. 2020 Sep 15;202:112475. doi: 10.1016/j.ejmech.2020.112475. Epub 2020 Jun 30. PMID: 32652406. 2. Vale N, Alves C, Sharma V, Lázaro DF, Silva S, Gomes P, Outeiro TF. A new MAP-Rasagiline conjugate reduces α-synuclein inclusion formation in a cell model. Pharmacol Rep. 2020 Apr;72(2):456-464. doi: 10.1007/s43440-019-00032-x. Epub 2020 Jan 15. PMID: 32048262.
In vivo protocol:	1. Kano O, Tsuda H, Hayashi A, Arai M. Rasagiline as Adjunct to Levodopa for Treatment of Parkinson's Disease: A Systematic Review and Meta-Analysis. Parkinsons Dis. 2022 Aug 30;2022:4216452. doi: 10.1155/2022/4216452. PMID: 36081594; PMCID: PMC9448622. 2. Oka H, Sengoku R, Nakahara A, Yamazaki M. Rasagiline does not exacerbate autonomic blood pressure dysregulation in early or mild Parkinson's disease. Clin Park Relat Disord. 2021 Dec 13;6:100124. doi: 10.1016/j.prdoa.2021.100124. PMID: 34977548; PMCID: PMC8689235.

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1: Cronin A, Grealy M. Neuroprotective and Neuro-restorative Effects of Minocycline and Rasagiline in a Zebrafish 6-Hydroxydopamine Model of Parkinson's Disease. Neuroscience. 2017 Dec 26;367:34-46. doi: 10.1016/j.neuroscience.2017.10.018. Epub 2017 Oct 24. PubMed PMID: 29079063.

2: Cereda E, Cilia R, Canesi M, Tesei S, Mariani CB, Zecchinelli AL, Pezzoli G. Efficacy of rasagiline and selegiline in Parkinson's disease: a head-to-head 3-year retrospective case-control study. J Neurol. 2017 Jun;264(6):1254-1263. doi: 10.1007/s00415-017-8523-y. Epub 2017 May 26. Erratum in: J Neurol. 2017 Aug 22;:. PubMed PMID: 28550482; PubMed Central PMCID: PMC5570795.

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