OR-1896,220246-81-1

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OR-1896

CAS No. : 220246-81-1

MCE 国际站：OR-1896

产品活性：OR-1896 是 Levosimendan 的活性长寿代谢产物。OR-1896 是一种高选择性磷酸二酯酶 (PDE III) 抑制剂，是一种功能强大的血管扩张剂。OR-1896 可以打开 ATP 敏感的 K⁺ 通道，并具有 Ca²⁺ 致敏作用。OR-1896 可减轻心肌细胞的凋亡，心脏重塑和心肌炎症。

研究领域：Membrane Transporter/Ion Channel  |  Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Potassium Channel  |  Phosphodiesterase (PDE)  |  Drug Metabolite  |  Apoptosis

In Vitro: There are many evidences has accumulated and revealed a variety of beneficial pleiotropic effects OR-1896. OR-1896 evokes prominent vasodilatory responses, activation of ATP-sensitive sarcolemmal K⁺ channels of smooth muscle cells appears as a powerful vasodilator mechanism. Additionally, activation of ATP-sensitive K⁺ channels in the mitochondria potentially extends the range of cellular actions towards the modulation of mitochondrial ATP production and implicates a pharmacological mechanism for cardioprotection.

In Vivo: During the metabolism of Levosimendan approximately 5% of the drug is converted to the metabolite OR-1855 in the large intestine, and then acetylated in the liver to form the active metabolite OR-1896. Binding to plasma proteins is 98% for Levosimendan but only 40% for OR-1896. Unlike Levosimendan, which has an elimination half-life of 1-1.5 h, the half-life of OR-1896 is about 75 to 80 h allowing cardiovascular effects to persist up to 7 to 9 days after discontinuation of a 24-hour infusion of levosimendan. The pharmacokinetic of the parent drug is unaltered in subjects with severe renal impairment or with moderate hepatic impairment, whereas the elimination of its metabolites (OR-1896) can be prolonged.

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