左西孟旦杂质
- CAS号:220246-81-1
- 英文名:(R)-N-Acetyl-6-(4-aminophenyl)-4,5-dihydro-5-methyl-3(2H)-pyridazinone
- 中文名:左西孟旦杂质
- CBNumber:CB11120951
- 分子式:C13H15N3O2
- 分子量:245.28
- MOL File:220246-81-1.mol
- 熔点 :224-226°C
- 密度 :1.27±0.1 g/cm3(Predicted)
- 储存条件 :-20°C Freezer
- 溶解度 :Acetone (Slightly), DMSO (Slightly), Methanol (Slightly)
- 形态 :Solid
- 酸度系数(pKa) :13.67±0.60(Predicted)
- 颜色 :Pale Yellow to Light Yellow
- CAS 数据库 :220246-81-1
左西孟旦杂质性质、用途与生产工艺
- 生物活性 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。
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靶点
PDE3/PDE Ⅲ
K+ Channel
Drug Metabolite
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体外研究
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.
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体内研究
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.
- 更新日期:2024/11/08
- 产品编号:HY-135746
- 产品名称:左西孟旦杂质 OR-1896
- CAS编号:220246-81-1
- 包装:5mg
- 价格:2800元
- 更新日期:2024/11/08
- 产品编号:HY-135746
- 产品名称:左西孟旦杂质 OR-1896
- CAS编号:220246-81-1
- 包装:10mM * 1mLin DMSO
- 价格:3080元
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