ChemicalBook > CAS DataBase List > Rasagiline mesylate

Rasagiline mesylate

Product Name
Rasagiline mesylate
CAS No.
161735-79-1
Chemical Name
Rasagiline mesylate
Synonyms
Azilect;RASAGILINE MESILATE;RASAGILINE GLUCURONIDE;CS-289;Agilect;TVP-101;TV 1012;TVP-1012;Unii-lh8C2ji290;RASAGILINE MESYLATE
CBNumber
CB7501001
Molecular Formula
C13H17NO3S
Formula Weight
267.34398
MOL File
161735-79-1.mol
More
Less

Rasagiline mesylate Property

Melting point:
155-158°C
storage temp. 
2-8°C
solubility 
H2O: ≥20mg/mL
form 
powder
color 
white to tan
optical activity
[α]/D +15 to +28°, c = 0.6 mg/mL in H2O
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO, distilled water or ethanol may be stored at -20°C for up to 1 month.
InChI
InChI=1/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)/t12-;/s3
InChIKey
JDBJJCWRXSVHOQ-ZLBVLXFENA-N
SMILES
C12C=CC=CC=1CC[C@H]2NCC#C.S(C)(O)(=O)=O |&1:8,r|
CAS DataBase Reference
161735-79-1(CAS DataBase Reference)
More
Less

Safety

Hazard Codes 
Xn
Risk Statements 
22
Safety Statements 
24/25
WGK Germany 
3
HS Code 
29214990
More
Less

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

Precautionary statements

P280Wear protective gloves/protective clothing/eye protection/face protection.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

More
Less

N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML0124
Product name
Rasagiline mesylate
Purity
≥98% (HPLC)
Packaging
10mg
Price
$107
Updated
2024/03/01
Sigma-Aldrich
Product number
SML0124
Product name
Rasagiline mesylate
Purity
≥98% (HPLC)
Packaging
50mg
Price
$431
Updated
2024/03/01
TCI Chemical
Product number
R0213
Product name
Rasagiline Mesylate
Packaging
250MG
Price
$84
Updated
2024/03/01
TCI Chemical
Product number
R0213
Product name
Rasagiline Mesylate
Packaging
5G
Price
$684
Updated
2024/03/01
TCI Chemical
Product number
R0213
Product name
Rasagiline Mesylate
Packaging
1G
Price
$228
Updated
2024/03/01
More
Less

Rasagiline mesylate Chemical Properties,Usage,Production

Description

Rasagiline mesylate is a potent and selective irreversible monoamine oxidase B (MAO-B) inhibitor launched in 2005 in Israel by Teva as monotherapy in patients with early Parkinson's disease and as adjuvant treatment in moderate-toadvanced disease. Lundbeck will market the drug throughout Europe. Rasagiline is in phase II clinical trials at Teva and Eisai for the treatment of Alzheimer's type dementia.

Chemical Properties

White to Off-White Crystalline Solid

Uses

A selective irreversible MAO-B inhibitor. Antiparkinsonian

Uses

Rasagiline Mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.

Uses

Rasagiline is a selective irreversible MAO-B inhibitor. Rasagiline is an Antiparkinsonian agent.

Indications

Rasagiline mesylate is a novel, potent, second-generation, selective, irreversible MAO-B inhibitor that blocks the breakdown of dopamine. It is approved for the treatment of PD. Indications for use of once-daily rasagiline are as a monotherapy in early PD and as an adjunct to levodopa in moderate to advanced disease. Rasagiline significantly improves symptoms during initial monotherapy in patients with early PD and as an adjunct treatment to levodopa in moderate-to-advanced patients. Rasagiline is well tolerated up to doses as high as 20 mg/day. Evidence for neuroprotective effect of rasagiline is as follows (Jain 2010c):
Structure activity studies have shown that the neuroprotective activity is associated with the propargyl moiety of rasagiline, which protects mitochondrial viability.
Experimental evidence supports rasagiline's neuroprotective efficacy, showing that neuronal survival is related to the anti-apoptotic properties of its propargyl moiety. Aminoindan metabolite of rasagiline has been shown to have neuroprotective properties (Bar-Am et al. 2010).

brand name

Azilect (Teva).

General Description

Rasagiline mesylate, (R)-N-(prop-2-ynyl)-2,3-dihydro-1H-inden-1-amine methanesulfonate(Azilect), belongs to the propargylamine family and is a whiteto off-white powder, soluble in water or ethanol, slightly solublein isopropanol. Rasagiline is rapidly absorbed. Plasmaprotein binding for rasagiline ranges from 88% to 94%, withspecific binding to serum albumin being 61% to 63%. It undergoescomplete biotransformation before excretion, mainlyvia N-dealkylation and hydroxylation, to yield three majormetabolites: 1(R)-aminoindan, 3-hydroxy-N-propargyl-1-aminoindan, and 3-hydroxy-1-aminoindan. Both oxidativepathways are catalyzed by cytochrome P450 (CYP) enzymes,mainly the 1A2 isozyme. Rasagiline and its metabolites undergoglucuronide conjugation with subsequent urinary excretion.Inhibitors of the CYP1A2 may increase plasmaconcentrations of rasagiline up to twofold. Because rasagilineis a selective and irreversible inhibitor of MAO-B, itsduration of action is independent of the drug’s half-life and isinstead determined by the regeneration rate of MAO-B. Thischaracteristic is potentially beneficial in PD, where rasagiline’sprolonged effect may be able to limit the fluctuating responsesthat are characteristic of long-term drug treatmentwith levodopa.

Biochem/physiol Actions

Rasagiline mesylate is an irreversible inhibitor of monoamine oxidase selective for MAO type B over type A by a factor of fourteen. It has anti-apoptotic and neuroprotectant activity and has been used as a treatment for Parkinson′s disease.

Mechanism of action

The specific mechanism of action of Rasagiline mesylate is unknown. One of these mechanisms is thought to be related to its MAO-B inhibitory activity, which leads to elevated extracellular dopamine levels in the striatum. It irreversibly blocks dopamine metabolism, thereby increasing dopamine levels, which can be beneficial for symptoms in Parkinson's disease patients.

Side effects

Rasagiline mesylate has been shown to be effective, safe and well tolerated as monotherapy in early Parkinson's disease. The most common are infection, headache, dizziness, weakness, anorexia and vomiting. In rare patients, it may cause new malignancies (melanoma and squamous cell carcinoma of the skin).

Synthesis

1-Indanone (122) was condensed with benzyl amine to give corresponding enamine which was reduced with sodium borohydride in ethanol to give racemic Nbenzyl- 1-inda-namine (123) in 82% yield. The racemic benzylamine 123 was resolved with L-tartaric acid and recrystallized from boiling water to give optical pure Rbenzylamine 124 as a tartarate salt. The recovered S-isomer 125 can be racemized under basic condition to give back as the starting racemic 123. Compound 124 was hydrogenated and basified to give free amine 126 in 72 % yield which was alkylated with propargyl chloride and K2CO3 in hot acetonitrile to yield free resagiline. Finally resagiline mesilate (XVII) was obtained by treating resagiline with methanesulfonic acid in refluxing IPA.

storage

room temperature (desiccate)

References

1) Youdim?et al.?(2001),?Rasagiline [N-propargyl-1R(+)-aminoindan], a selective and potent inhibitor of mitochondrial monoamine oxidase B; Br. J. Pharmacol.,?132?500 2) Cereda?et al.?(2017),?Efficacy of rasagiline and selegiline in Parkinson’s disease: a head-to-head 3-year retrospective case-control study; J. Neurol.,?264?1254 3) Cronin and Grealy (2017),?Neuroprotective and Neuro-restorative Effects of Minocycline and Rasagiline in Zebrafish 6-Hydroxydopamine Model of Parkinson’s Disease; Neuroscience,?367?34 4) Kang?et al.?(2017),?TrkB neurotrophic activities are blocked by α-synuclein, triggering dopaminergic cell death in Parkinson’s disease; Proc. Natl. Acad. Sci. USA,?114?10773 5) Ledreux?et al.?(2016),?BDNF levels are increased by aminoindan and rasagiline in a double lesion model of Parkinson’s disease; Brain Res.,?1631?34

Rasagiline mesylate Preparation Products And Raw materials

Raw materials

Preparation Products

More
Less

Rasagiline mesylate Suppliers

Beijing Mesochem Technology Co., Ltd.
Tel
010-57862036 18811083386
Email
msales@mesochem.com
Country
China
ProdList
205
Advantage
58
Taizhou Yuxin Biotechnology Co., Ltd.,
Tel
+86-0576--88902229 +86-13968687450
Email
yuxin@yuxchem.com
Country
China
ProdList
209
Advantage
58
Zhejiang Jiuzhou Pharmaceutical Co., Ltd
Tel
13566413511
Email
le.sun@jiuzhoupharma.com
Country
China
ProdList
31
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
96815
Advantage
76
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
JinYan Chemicals(ShangHai) Co.,Ltd.
Tel
13817811078
Fax
86-021-50426522,50426273
Email
sales@jingyan-chemical.com
Country
China
ProdList
9976
Advantage
60
Jia Xing Isenchem Co.,Ltd
Tel
0573-85285100 18627885956
Fax
0573-85285100
Email
isenchem@163.com
Country
China
ProdList
9513
Advantage
66
Adamas Reagent, Ltd.
Tel
400-6009262 16621234537
Fax
021-64823266
Email
chenyj@titansci.com
Country
China
ProdList
14103
Advantage
59
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
19179
Advantage
64
Chemsky(shanghai)International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
Country
China
ProdList
32321
Advantage
50
XiaoGan ShenYuan ChemPharm co,ltd
Tel
15527768850
Email
1791901229@qq.com
Country
China
ProdList
8836
Advantage
52
Nanjing Chemipioneer Pharma& Tech Co., LTD
Tel
025-52643182 13914798241
Fax
025-52643182
Email
zhoulq@chemipioneer.com.cn
Country
China
ProdList
80
Advantage
62
Hangzhou Yuhao Chemical Technology Co., Ltd
Tel
0571-82693216
Fax
+86-571-82880190
Email
info@yuhaochemical.com
Country
China
ProdList
9387
Advantage
52
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4727
Advantage
58
BioBioPha Co., Ltd.
Tel
0871-65217109 13211707573;
Fax
0871-65215563
Email
y.liu@mail.biobiopha.com
Country
China
ProdList
5653
Advantage
65
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Tel
0755-4000505016 13380397412
Fax
0755 28094224
Email
3001272453@qq.com
Country
China
ProdList
5047
Advantage
50
Beijing HuaMeiHuLiBiological Chemical
Tel
010-56205725
Fax
010-65763397
Email
waley188@sohu.com
Country
China
ProdList
12335
Advantage
58
Shanghai T&W Pharmaceutical Co., Ltd.
Tel
+86 21 61551611
Fax
+86 21 50676805
Country
China
ProdList
9891
Advantage
58
Nanjing Norris-Pharm Technology Co., Ltd
Tel
13901585132
Fax
+86-25-52131256
Email
799750417@qq.com
Country
China
ProdList
8878
Advantage
55
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7552
Advantage
61
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Fax
021-50323701
Email
market@aladdin-e.com
Country
China
ProdList
25003
Advantage
65
China Nobel Chem Co., Limited
Tel
+86(0)21 60484900
Fax
+86(0)21 60484900
Country
China
ProdList
764
Advantage
50
Cantotech Chemicals, Ltd.
Tel
86-0755-86635001
Fax
86-0755-22642228
Email
cantotech@126.com
Country
China
ProdList
4566
Advantage
55
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3239
Advantage
55
TargetMol Chemicals Inc.
Tel
021-021-33632979 15002134094
Fax
021-33632979
Email
marketing@targetmol.com
Country
China
ProdList
7783
Advantage
58
Wuhan DKY Technology Co.,Ltd.
Tel
27-81302488 18007166089
Fax
027-81302088
Email
info@dkybpc.com
Country
China
ProdList
2024
Advantage
58
Hubei XinyuanShun Chemical Co., Ltd.
Tel
13971561712, 13995564702, 027-50664929
Fax
027-50664927
Email
hbeixys2001@163.com
Country
China
ProdList
3120
Advantage
55
Bide Pharmatech Ltd.
Tel
400-164-7117 13681763483
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
41462
Advantage
60
Suzhou yacoo science co.,Ltd
Tel
0512-87182056 18013166090
Fax
0512-87182056
Email
lingling.qi@yacoo.com.cn
Country
China
ProdList
7295
Advantage
60
Shanghai Xingui Biotechnology Co., Ltd.
Tel
17501653715
Email
xingui2022@126.com
Country
China
ProdList
10015
Advantage
58
Shanghai Kewel Chemical Co., Ltd.
Tel
021-64609169 18901607656
Fax
021-64609160
Email
greensnown@163.com
Country
China
ProdList
9906
Advantage
50
Hangzhou J&H Chemical Co., Ltd.
Tel
0571-+86-571-87396432
Fax
0571-87396431
Email
sales@jhechem.com
Country
China
ProdList
11578
Advantage
59
Shanghai HuanChuan Industry Co.,Ltd.
Tel
021-61478794
Fax
021-61478794
Email
sales@hcshhai.com
Country
China
ProdList
9793
Advantage
50
AdooQ Bioscience CHINA
Tel
025-58849295 18951903616;
Fax
025-68650336
Email
info@adooq.cn
Country
China
ProdList
2990
Advantage
60
Credit Asia Chemical Co., Ltd.
Tel
+86 (21) 61124340
Fax
+86 (21) 6129-4103
Country
China
ProdList
9756
Advantage
58
Hubei Jusheng Technology Co.,Ltd
Tel
027-59599241 18871490274
Fax
027-59599241
Email
1400878000@qq.com
Country
China
ProdList
9958
Advantage
58
LETOPHARM LIMITED
Tel
+86-21-5821 5861
Fax
+86-21-5106 2861
Email
sales@letopharm.com
Country
China
ProdList
2384
Advantage
58
Chizhou Kailong Import and Export Trade Co., Ltd.
Tel
Fax
-
Email
xg01_gj@163.com
Country
China
ProdList
9484
Advantage
50
Sigma-Aldrich
Tel
021-61415566 800-8193336
Email
orderCN@merckgroup.com
Country
China
ProdList
51456
Advantage
80
Nanjing XiZe Biotechnology CO., Ltd.
Tel
025-66023220 0086-15250997978
Fax
025-58362220
Email
1511893459@qq.com
Country
China
ProdList
7850
Advantage
55
Nanjing Chempioneer Pharmaceutical Co., Ltd.
Tel
18068075658
Fax
-
Email
sales@chempioneer.com
Country
China
ProdList
1811
Advantage
58
Struchem Co., Ltd.
Tel
0512-0512-63009836 15365350169
Fax
0512-63006936
Email
helen@struchem.com
Country
China
ProdList
3984
Advantage
60
Wuhan ChemFaces Biochemical Co., Ltd.
Tel
18607101326 15172504745
Fax
+86-27-84254680
Email
aileen@chemfaces.com
Country
China
ProdList
7057
Advantage
55
Codow Chemical Co.,Ltd.
Tel
18620099427
Fax
+86-20-62619665
Email
amy@howeipharm.com
Country
China
ProdList
17687
Advantage
55
Pharmacodia (Beijing) Co.,Ltd
Tel
+86-400-851-9921
Fax
+86-10-82826195
Email
sales@pharmacodia.com
Country
China
ProdList
2317
Advantage
55
Henan CoreyChem Co., Ltd
Tel
0371-86658258
Fax
0371-60996044
Email
info@coreychem.com
Country
China
ProdList
10453
Advantage
58
Beijing Cooperate Pharmaceutical Co.,Ltd
Tel
+86-010-60279497 +86-15646567669
Fax
010-60279497
Email
sales01@cooperate-pharm.com
Country
China
ProdList
137
Advantage
58
Guangzhou QiYun Biotechnology Co., Ltd.
Tel
020-61288194 61288195
Fax
020-61288700
Email
505721671@qq.com
Country
China
ProdList
3866
Advantage
58
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
27313
Advantage
60
More
Less

View Lastest Price from Rasagiline mesylate manufacturers

BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
Product
Rasagiline Mesylate 161735-79-1
Price
US $0.00/g
Min. Order
1g
Purity
More Than 99%
Supply Ability
100kg/Month
Release date
2024-09-25
Zhuozhou Wenxi import and Export Co., Ltd
Product
Rasagiline mesylate 161735-79-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Rasagiline mesylate 161735-79-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-08

161735-79-1, Rasagiline mesylateRelated Search:


  • (1R)-2,3-Dihydro-N-2-propynyl-1H-inden-1-amine methanesulfonate
  • CS-289
  • R-(+)-Rasagiline mesylate
  • N-(prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-amine methanesulfonate
  • Rasagiline Mesylate/Tartrate/Base
  • (1R)-2,3-Dihydro-N-2-propyn-1-yl-1H-inden-1-amine Mesylate
  • (R)-N-2-Propynyl-1-indanamine Mesylate
  • Agilect
  • Azilect
  • TVP-101
  • RASAGILINE MESYLATE
  • (r)-n-2-propynyl-1-indanamine methanesulfonate
  • Rasagiline nesylate
  • RASAGILINE MESILATE
  • TVP-1012
  • (R)-2,3-Dihydro-N-2-propynyl-1-indenaMine Mesylate
  • TV 1012
  • (R)-N-(Prop-2-yn-1-yl)-2,3-dihydro-1H-inden-1-aMine Methanesulfonate
  • RASAGILINE GLUCURONIDE
  • (1R)-2,3-dihydro-N-2-propyn-1-yl-1H-inden-1-amine,methanesulfonate (1:1)
  • (1R)-2,3-Dihydro-N-2-propynl-1H-inden-1-amine methanesulfonate
  • N-Propargyl-1(R)-aminoindan methanesulfonate
  • 1H-Inden-1-amine, 2,3-dihydro-N-2-propynyl-, (R)-, methanesulfonate
  • Rasagiline methanesulfonate
  • Unii-lh8C2ji290
  • 1H-Inden-1-amine, 2,3-dihydro-N-2-propyn-1-yl-, (1R)-, methanesulfonate (1:1)
  • (R)-N-(2-Propyn-1-yl)-1-indanamine Methanesulfonate
  • (R)-N-Propargyl-1-indanamine Methanesulfonate
  • Rasagiline mesylate USP/EP/BP
  • Rasagiline Mesylate(pure)
  • Rasagiline MesylateQ: What is Rasagiline Mesylate Q: What is the CAS Number of Rasagiline Mesylate Q: What is the storage condition of Rasagiline Mesylate Q: What are the applications of Rasagiline Mesylate
  • (1R)-N-prop-2-ynylindan-1-amine
  • Resagiline mesylate
  • 161735-79-1
  • 136235-79-1
  • 161735-79-5
  • C12H13NCH4O3S
  • Chiral
  • Chiral Reagents
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Rasagiline
  • Signalling
  • APIs
  • 161735-79-1