Sarpogrelate hydrochloride

製品コードS3706 バッチS370601

印刷

化学情報

Chemical Structure Synonyms MCI-9042 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H31NO6.HCl
分子量 465.97 CAS No. 135159-51-2
Solubility (25°C)* 体外 DMSO 93 mg/mL (199.58 mM)
Water 93 mg/mL (199.58 mM)
Ethanol 30 mg/mL (64.38 mM)
* <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 Sarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively.
in vitro Sarpogrelate inhibits thrombus formation, lowers platelet aggregation, inhibits both serotonin-induced coronary artery spasm and contraction in porcine model as well as vascular smooth muscle cell proliferation. Sarpogrelate exibit specificity toward 5-HT2 receptors, since it has lack of significant 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 antagonistic activity[1]. Sarpogrelate specifically inhibited the serotonin-induced cytokine trigger but did not influence platelet-derived growth factor–, endothelin–, or angiotensin II–induced cell proliferation. Sarpogrelate inhibited the serotonin-induced increase in intracellular free ionized calcium concentration, prevented mitogen-activated protein kinase activation, and down-regulated expression of the protooncogenes c-fos and c-jun. Sarpogrelate acted at the G1 phase of the cell cycle[2].
in vivo Sarpogrelate can fully protect albino BALB/c retinas, both structurally and functionally, from light-induced retinopathy[3]. It is used clinically for the treatment of vascular inflammation and atherosclerosis. Sarpogrelate mitigates albuminuria in diabetic nephropathy by hindering glomerular platelet activation. Sarpogrelate ameliorates diabetic nephropathy not only by suppressing macrophage infiltration, but also by anti-inflammatory and anti-fibrotic effects[4].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Porcine coronary artery smooth muscle cells
濃度 1 μmol/L
反応時間 96 h
実験の流れ Cell number was measured using a Coulter counter 96 hours after treatment in the absence and in the presence of sarpogrelate (1 μmol/L).
動物実験 動物モデル BALB/c mice
投薬量 5, 15, 30, 40, or 50 mg/kg
投与方法 i.p.

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。