Prasugrel

製品コードS1258 バッチS125803

印刷

化学情報

 Chemical Structure Synonyms Effient, Efient, Prasita,CS-747, LY640315,PCR 4099 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C20H20FNO3S

分子量 373.44 CAS No. 150322-43-3
Solubility (25°C)* 体外 DMSO 33 mg/mL (88.36 mM)
Ethanol 8 mg/mL (21.42 mM)
Water Insoluble
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.
* <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 Prasugrel (Effient、Efient、Prasita、CS-747、LY640315、PCR 4099) は、血栓性心血管イベントの減少に使用されるチエノピリジンADP receptor (P2Y12)アンタゴニストです。
in vitro

This compound is a novel orally active thienopyridine with faster, higher and more reliable inhibition of platelet aggregation than clopidogrel reflecting its metabolism in vivo to an active metabolite with selective P2Y(12) antagonistic activity.

in vivo

Prasugrel shows platelet inhibition that was 8.2 times more potent than clopidogrel in WT mice. This compound (3 and 10 mg/kg) dose-relatedly and significantly reduces thrombus-mediated cerebral infarction 24 hours after the irradiation in rat models of cerebral and peripheral arterial occlusive diseases. It (0.3-3 mg/kg) reduces incidence, total area, and total number of cerebral infarcts in a dose-related manner 24 hours after the vascular injury in an embolic infarction rats model. This chemical (0.03-3 mg/kg/day) administered from the day before the lauric acid injection for 11 successive days inhibits the progression of the disease in a dose-related manner in rats with lauric acid-induced peripheral arterial occlusive diseases. It administrated in dogs (0.03-0.3 mg/kg/day) and monkeys (0.1 and 0.3 mg/kg/day) once a day for 14 days results in potent, dose-related and cumulative inhibition of ADP-induced platelet aggregation. This compound (0.1-1 mg/kg/day, p.o.) significantly prolongs the time to arterial occlusion and increases the duration of arterial patency in a rat model of electrically-induced arterial thrombosis.

プロトコル(参考用のみ)

参考

  • https://pubmed.ncbi.nlm.nih.gov/17681285/
  • https://pubmed.ncbi.nlm.nih.gov/19356727/
  • https://pubmed.ncbi.nlm.nih.gov/12714600/

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:

Effect of RAD51C expression on the chemosensitivity of Eμ-Myc p19Arf-/- cells and its clinical significance in breast cancer [ Oncol Lett, 2018, 15(5):6107-6114] PubMed: 29731842
Evaluation system for arrhythmogenic potential of drugs using human-induced pluripotent stem cell-derived cardiomyocytes and gene expression analysis [Higa A, et al. J Toxicol Sci, 2017, 42(6):755-761] PubMed: 29142174

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。