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MedKoo Cat#: 318653 | Name: Rasagiline Mesylate
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Description:

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

Rasagiline Mesylate is a selective irreversible MAO-B inhibitor. Rasagiline Mesylate displays anti-Parkinsonian activity, exhibits neuroprotective and antiapoptotic activity against several neurotoxins in cell culture.

Chemical Structure

Rasagiline Mesylate
Rasagiline Mesylate
CAS#161735-79-1 (mesylate)

Theoretical Analysis

MedKoo Cat#: 318653

Name: Rasagiline Mesylate

CAS#: 161735-79-1 (mesylate)

Chemical Formula: C13H17NO3S

Exact Mass: 0.0000

Molecular Weight: 267.34

Elemental Analysis: C, 58.40; H, 6.41; N, 5.24; O, 17.95; S, 11.99

Price and Availability

Size Price Availability Quantity
100mg USD 650.00
200mg USD 950.00
500mg USD 1,450.00
1g USD 2,450.00
2g USD 3,950.00
5g USD 6,450.00
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Related CAS #
136236-51-6 (free base) 161735-79-1 (mesylate) 136236-52-7 (tartrate)
Synonym
Rasagiline Mesylate; Azilect; TVP-1012; Rasagiline mesilate; Agilect; TVP-1022; TVP1022; TVP-101; AGN 1135; AGN-1135; Azilect; N-2-propynyl-1-indanamine N-propargyl-1-aminoindan mesylate; rasagiline; rasagiline hydrochloride; TVP 101; TVP 1022;
IUPAC/Chemical Name
N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate
InChi Key
JDBJJCWRXSVHOQ-UHFFFAOYSA-N
InChi Code
InChI=1S/C12H13N.CH4O3S/c1-2-9-13-12-8-7-10-5-3-4-6-11(10)12;1-5(2,3)4/h1,3-6,12-13H,7-9H2;1H3,(H,2,3,4)
SMILES Code
CS(=O)(=O)O.C#CCNC1CCC2=CC=CC=C12
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, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
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
More Info
Product Data
Product Data
Instruction
View handling instruction
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/
Solvent mg/mL mM
Solubility
DMSO 26.7 100.00
Water 26.7 100.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 267.34 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.

Recalculate based on batch purity %
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.
1: Müller T. Pharmacokinetic/pharmacodynamic evaluation of rasagiline mesylate for Parkinson's disease. Expert Opin Drug Metab Toxicol. 2014 Oct;10(10):1423-32. doi: 10.1517/17425255.2014.943182. Epub 2014 Sep 6. PMID: 25196265. 2: Nagai M, Hattori N. [Pharmacological properties and clinical efficacy of rasagiline mesylate (Azilect®)]. Nihon Yakurigaku Zasshi. 2020;155(3):187-194. Japanese. doi: 10.1254/fpj.19146. PMID: 32378642. 3: Mahde BW, Abbas Hussein A, Sahib AS. Preparation and in vitro Evaluation of Rasagiline Mesylate Hybrid Nanoparticles. Arch Razi Inst. 2023 Jun 30;78(3):1023-1028. doi: 10.22092/ARI.2022.360193.2563. PMID: 38028832; PMCID: PMC10657949. 4: Mahde BW, Abbas Hussein A, Alsaraf KM, Abdelamir Mohammad H. Transdermal Microneedle-Mediated Delivery of Rasagiline Nanoparticles. Arch Razi Inst. 2023 Jun 30;78(3):1017-1022. doi: 10.22092/ARI.2022.360192.2562. PMID: 38028835; PMCID: PMC10657957. 5: Rabey JM, Sagi I, Huberman M, Melamed E, Korczyn A, Giladi N, Inzelberg R, Djaldetti R, Klein C, Berecz G; Rasagiline Study Group. Rasagiline mesylate, a new MAO-B inhibitor for the treatment of Parkinson's disease: a double-blind study as adjunctive therapy to levodopa. Clin Neuropharmacol. 2000 Nov- Dec;23(6):324-30. doi: 10.1097/00002826-200011000-00005. PMID: 11575866. 6: Guay DR. Rasagiline (TVP-1012): a new selective monoamine oxidase inhibitor for Parkinson's disease. Am J Geriatr Pharmacother. 2006 Dec;4(4):330-46. doi: 10.1016/j.amjopharm.2006.12.001. PMID: 17296539. 7: Varela A, Mavroidis M, Katsimpoulas M, Sfiroera I, Kappa N, Mesa A, Kostomitsopoulos NG, Cokkinos DV. The neuroprotective agent Rasagiline mesylate attenuates cardiac remodeling after experimental myocardial infarction. ESC Heart Fail. 2017 Aug;4(3):331-340. doi: 10.1002/ehf2.12140. Epub 2017 Mar 12. PMID: 28772050; PMCID: PMC5542732. 8: Ali MM, Shoukri RA, Yousry C. Thin film hydration versus modified spraying technique to fabricate intranasal spanlastic nanovesicles for rasagiline mesylate brain delivery: Characterization, statistical optimization, and in vivo pharmacokinetic evaluation. Drug Deliv Transl Res. 2023 Apr;13(4):1153-1168. doi: 10.1007/s13346-022-01285-5. Epub 2022 Dec 30. PMID: 36585559; PMCID: PMC9981512. 9: Dugarte-Dugarte AJ, Toro RA, van de Streek J, Henao JA, Fitch AN, Dejoie C, Delgado JM, Díaz de Delgado G. Hydrogen bonding patterns and C-H...π interactions in the structure of the antiparkinsonian drug (R)-rasagiline mesylate determined using laboratory and synchrotron X-ray powder diffraction data. Acta Crystallogr B Struct Sci Cryst Eng Mater. 2023 Dec 1;79(Pt 6):462-472. doi: 10.1107/S2052520623007758. Epub 2023 Oct 11. PMID: 37820013; PMCID: PMC10833353. 10: Patel P, Pol A, Kalaria D, Date AA, Kalia Y, Patravale V. Microemulsion- based gel for the transdermal delivery of rasagiline mesylate: In vitro and in vivo assessment for Parkinson's therapy. Eur J Pharm Biopharm. 2021 Aug;165:66-74. doi: 10.1016/j.ejpb.2021.04.026. Epub 2021 May 7. PMID: 33971272. 11: ElShagea HN, Makar RR, Salama AH, Elkasabgy NA, Basalious EB. Investigating the Targeting Power to Brain Tissues of Intranasal Rasagiline Mesylate-Loaded Transferosomal In Situ Gel for Efficient Treatment of Parkinson's Disease. Pharmaceutics. 2023 Feb 5;15(2):533. doi: 10.3390/pharmaceutics15020533. PMID: 36839855; PMCID: PMC9967009. 12: Rohith G, Satheesha Babu BK. Influence of chitosan thioglycolic acid conjugate in improving bioavailability of an antiparkinson drug; Rasagiline Mesylate from transdermal patch. Drug Dev Ind Pharm. 2021 Jun;47(6):963-976. doi: 10.1080/03639045.2021.1957919. Epub 2021 Aug 2. PMID: 34283682. 13: Fernández M, Barcia E, Fernández-Carballido A, Garcia L, Slowing K, Negro S. Controlled release of rasagiline mesylate promotes neuroprotection in a rotenone-induced advanced model of Parkinson's disease. Int J Pharm. 2012 Nov 15;438(1-2):266-78. doi: 10.1016/j.ijpharm.2012.09.024. Epub 2012 Sep 15. PMID: 22985602. 14: Pingili R, Vemulapalli S, Mullapudi SS, Nuthakki S, Pendyala S, Kilaru N. Pharmacokinetic interaction study between flavanones (hesperetin, naringenin) and rasagiline mesylate in wistar rats. Drug Dev Ind Pharm. 2016;42(7):1110-7. doi: 10.3109/03639045.2015.1115868. Epub 2015 Nov 30. PMID: 26530401. 15: Shelke PG, Chandewar AV. Study of stress degradation behavior of rasagiline mesylate under hydrolytic conditions by high performance liquid chromatography. Drug Res (Stuttg). 2014 Apr;64(4):182-5. doi: 10.1055/s-0033-1355332. Epub 2013 Sep 18. PMID: 24048951. 16: Ravi PR, Aditya N, Cherian L, Patil S. LC method for determination of rasagiline mesylate in different plasma matrices and its application to oral pharmacokinetic study in rabbits. J Chromatogr Sci. 2013 Jan;51(1):1-7. doi: 10.1093/chromsci/bms096. Epub 2012 Jun 11. PMID: 22689899. 17: Meier-Davis SR, Dines K, Arjmand FM, Hamlin R, Huang B, Wen J, Christianson C, Shudo J, Nagata T. Comparison of oral and transdermal administration of rasagiline mesylate on human melanoma tumor growth in vivo. Cutan Ocul Toxicol. 2012 Dec;31(4):312-7. doi: 10.3109/15569527.2012.676119. Epub 2012 Apr 20. PMID: 22515841. 18: Jiang Y, Zhang X, Mu H, Hua H, Duan D, Yan X, Wang Y, Meng Q, Lu X, Wang A, Liu W, Li Y, Sun K. Preparation and evaluation of injectable Rasagiline mesylate dual-controlled drug delivery system for the treatment of Parkinson's disease. Drug Deliv. 2018 Nov;25(1):143-152. doi: 10.1080/10717544.2017.1419514. PMID: 29275639; PMCID: PMC6058670. 19: Kanwar N, Bhandari R, Kuhad A, Sinha VR. Polycaprolactone-based neurotherapeutic delivery of rasagiline targeting behavioral and biochemical deficits in Parkinson's disease. Drug Deliv Transl Res. 2019 Oct;9(5):891-905. doi: 10.1007/s13346-019-00625-2. PMID: 30877626. 20: Ravi PR, Aditya N, Patil S, Cherian L. Nasal in-situ gels for delivery of rasagiline mesylate: improvement in bioavailability and brain localization. Drug Deliv. 2015;22(7):903-10. doi: 10.3109/10717544.2013.860501. Epub 2013 Nov 29. PMID: 24286183; PMCID: PMC11132615.