Rasagiline mesylate
- CAS No.
- 161735-79-1
- Chemical Name:
- Rasagiline mesylate
- Synonyms
- Azilect;RASAGILINE MESILATE;RASAGILINE GLUCURONIDE;CS-289;TVP-101;Agilect;TV 1012;TVP-1012;Unii-lh8C2ji290;RASAGILINE MESYLATE
- CBNumber:
- CB7501001
- Molecular Formula:
- C13H17NO3S
- Molecular Weight:
- 267.34398
- MOL File:
- 161735-79-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/1/10 13:59:45
| 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) |
Rasagiline mesylate price More Price(5)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich(India) | SML0124 | Rasagiline mesylate ≥98% (HPLC) | 161735-79-1 | 10MG | ₹10835.83 | 2022-06-14 | Buy |
| Sigma-Aldrich(India) | SML0124 | Rasagiline mesylate ≥98% (HPLC) | 161735-79-1 | 50MG | ₹43527.33 | 2022-06-14 | Buy |
| TCI Chemicals (India) | R0213 | Rasagiline Mesylate | 161735-79-1 | 250MG | ₹4500 | 2022-05-26 | Buy |
| TCI Chemicals (India) | R0213 | Rasagiline Mesylate | 161735-79-1 | 1G | ₹9700 | 2022-05-26 | Buy |
| TCI Chemicals (India) | R0213 | Rasagiline Mesylate | 161735-79-1 | 5G | ₹26400 | 2022-05-26 | Buy |
Rasagiline mesylate Chemical Properties,Uses,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
Rasagiline Mesylate is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
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).
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.
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).
Rasagiline mesylate Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| SGMR PHARMACEUTICALS PVT LTD | +91-9032001889 +91-9032001889 | Telangana, India | 83 | 58 | Inquiry |
| USV Pvt Ltd | +91-2267861111 +91-2225564048 | Maharashtra, India | 36 | 58 | Inquiry |
| Apotex Pharmachem India Pvt Ltd | +91-8022891034 +91-8022891000 | Karnataka, India | 109 | 58 | Inquiry |
| Glenmark Pharmaceuticals Limited | +912240189999 | Maharashtra, India | 93 | 58 | Inquiry |
| Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
| Nosch Labs Pvt Ltd | +91-4048557474 +91-9948222287 | Hyderabad, India | 58 | 58 | Inquiry |
| Orchid Pharma Ltd. (Formerly Known as Orchid Chemicals and Pharmaceuticals Ltd.) | +91-4428244254 +91-4428244254 | Tamil Nadu, India | 28 | 58 | Inquiry |
| Indoco Remedies Ltd | +91-2262871000 +91-2262871000 | Gujarat, India | 27 | 58 | Inquiry |
| Mylan Laboratories Ltd | +91-4023550543 +91-4030866666 | Telangana, India | 150 | 58 | Inquiry |
| Ralington Pharma | +91-7948911722 +91-9687771722 | Gujarat, India | 1350 | 58 | Inquiry |
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