Rasagiline Mesylate - 10mM in DMSO , Monoamine oxidase B inhibitor, CAS No.161735-79-1, Monoamine oxidase B inhibitor

CAS: 161735-79-1 Cat. No.: R409148 Peso molecular: 267.34 Número EC: 694-423-3 PubChem CID: 3052775

GRADE & PURITY 10mM in DMSO

Synonyms

TVP-1012 | (1R)​-2,​3-​dihydro-​N-​2-​propyn-​1-​yl-1H-​inden-​1-​amine,methanesulfonate (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson's disease.
In vitro

Rasagiline inhibits rat brain MAO type B and type A with IC50 of 4.43 nM and 412 nM, respectively. Rasagiline is three to 15 times more potent than selegiline for inhibition of MAO-B in rat brain and liver in vivo on acute and chronic administration, but has similar potency in vitro. Rasagiline prevents nuclear accumulation of GAPDH induced by N-methyl(R) salsolinol in SH-SY5Y cells. Rasagiline prevents the collapse in ΔΨm, and following apoptotic process, which indicates that mitochondria may determine the survival and death of the cells. Rasagiline has potent antiapoptotic and neuroprotective activities in response to serum and NGF withdrawal in partially neuronally differentiated PC12 cells and prevents the fall in mitochondrial membrane potential, the first step in cell death. Rasagiline is metabolized to its major metabolite aminoindan, selegiline gives rise to L-methamphetamine. Rasagiline directly activates PKC-MAP kinase pathway by a concentration and time dependent phosphorylation of p42 and p44 MAP kinase.

In vivo

Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. Rasagiline (0.2 mg/kg and 1 mg/kg) accelerates the recovery of motor function and spatial memory and reduces the cerebral oedema by about 40-50% in the mouse.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

TVP-1012 | (1R)​-2, ​3-​dihydro-​N-​2-​propyn-​1-​yl-1H-​inden-​1-​amine, methanesulfonate (1:1)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Rasagiline Mesylate (TVP-1012) is a new MAO-B inhibitor for the treatment of idiopathic Parkinson\'s disease.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

INHIBITOR

Mecanismo de acción

Monoamine oxidase B inhibitor

Nombres e identificadores

• Isómeros SMILES: CS(=O)(=O)O.C#CCN[C@@H]1CCC2=CC=CC=C12
• WGK Alemania: 3
• PubChem CID: 3052775
• Peso molecular: 267.34

Objetivos asociados (humanos)

MAOB Tclin Amine oxidase [flavin-containing] B (2 Activities)

Discover Target: MAOB

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A (1 Activities)

Discover Target: MAOA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: 2 mg/mL (5.74 mM); Water: Insoluble; Ethanol: Insoluble
• Rotación específica [α]: 21° (C=2,EtOH)
• Punto de fusión (°C): 157 °C