Rasagiline Mesylate

製品コードS2102 バッチS210201

印刷

化学情報

Chemical Structure Synonyms TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C12H13N.CH4O3S
分子量 267.34 CAS No. 161735-79-1
Solubility (25°C)* 体外 DMSO 53 mg/mL (198.24 mM)
Water 53 mg/mL (198.24 mM)
Ethanol 53 mg/mL (198.24 mM)
体内 （毎回新しく調製した物を用意してください）
Clear solution
Saline
30.0mg/ml Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Rasagiline Mesylate (TVP-1012,(R)-AGN1135 mesylate,TVP1012 mesylate) 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. [1] 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. [2] 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. [3] 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. [4]
in vivo

Rasagiline ex vivo inhibits MAO in the brain and liver with ED50 of 4.43 nM and 412 nM, respectively. [1] 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. [5]

プロトコル(参考用のみ)

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

A monoamine oxidase B inhibitor ethyl ferulate suppresses microglia-mediated neuroinflammation and alleviates ischemic brain injury [ Front Pharmacol, 2022, 13:1004215] PubMed: 36313349
Histamine signaling and metabolism identify potential biomarkers and therapies for lymphangioleiomyomatosis [ EMBO Mol Med, 2021, e13929] PubMed: 34378323

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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