Safinamide

製品コードS5357 バッチS535701

印刷

化学情報

Synonyms

EMD-1195686, PNU-15774E

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₇H₁₉FN₂O₂

分子量

302.34

CAS No.

133865-89-1

Solubility (25°C)*

体外

DMSO

60 mg/mL (198.45 mM)

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.000mg/ml (9.92mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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	Safinamide (EMD-1195686, PNU-15774E) is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.
in vitro	The antiparkinson mechanism of safinamide is through reversible inhibition of selective MAO-B, thus reducing the degradation of dopamine. It inhibits glutamate release and dopamine reuptake in the brain. This compound also blocks sodium and calcium channels^[2].
in vivo	Safinamide is absorbed quickly, with a bioavailability of 95%, and a demonstrated time to maximum plasma concentration of 1.8-2.8 hours. It exhibits extensive extravascular distribution with a volume of distribution of approximately 165 L. This compound does not undergo significant first-pass metabolism and is mediated by amidase enzymes producing safinamide acid and other metabolites. It is mediated by cytochrome P450 (CYP) 3A4 isoenzymes. It is 88% to 90% plasma protein-bound and is primarily eliminated through the kidneys (approximately 76%) in the form of its metabolites, with an elimination half-life of 20 to 30 hours. About 1.5% of this chemical is found excreted in the feces. It exhibits linear pharmacokinetics after oral administration of 50 mg to 300 mg (three times the maximum recommended daily dose) with a steady state reached within five to six days^[2].

プロトコル(参考用のみ)

参考

https://pubmed.ncbi.nlm.nih.gov/25600407/
https://pubmed.ncbi.nlm.nih.gov/29018297/

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。