OR-1896 ≥98%
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| 包装规格: | 5mg 10mg 25mg in glass bottle |
| 溶解性: | 溶于DMSO(62.5 mg/mL 超声) |
| 产品描述: | 基本信息 产品编号: O10212 产品名称: OR-1896 CAS: 220246-81-1 储存条件 粉末 -20℃ 四年 分子式: C13H15N3O2 溶于液体 -80℃ 6个月 分子量: 245.28 -20℃ 1个月 化学名: (R)-N-ACETYL-6-(4-AMINOPHENYL)-4,5-DIHYDRO-5-METHYL-3(2H)-PYRIDAZINONE Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 4.0770mL 20.3849mL 40.7697mL 5mM 0.8154mL 4.0770mL 8.1539mL 10mM 0.4077mL 2.0385mL 4.0770mL 生物活性 产品描述 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。 靶点 PDE3/PDE Ⅲ K+ Channel Drug Metabolite 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. 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 1-1.5h,the half-life of OR-1896 is about 75 to 80h 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. |
| 保存条件: | -20℃ |
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