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NSP-805

目录号: PL09737 纯度: ≥99%

NSP-805 是一种有效的，选择性的 phosphodiesterase 3 (PDE3) 抑制剂，为一种强心剂，具有舒张血管的作用。

CAS No. :125068-54-4

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中文名称	NSP-805
英文名称	NSP-805
英文别名	3(2H)-Pyridazinone,4,5-dihydro-5-methyl-6-[4-[(2-methyl-3-oxo-1-cyclopenten-1-yl)amino]phenyl]-;4-methyl-3-[4-[(2-methyl-3-oxocyclopenten-1-yl)amino]phenyl]-4,5-dihydro-1H-pyridazin-6-one;NSP 805;NSP-805;3(2H)-Pyridazinone, 4,5-dihydro-5-methyl-6-(4-((2-methyl-3-oxo-1-cyclopenten-1-yl)amino)phenyl)-;4,5-Dihydro-5-methyl-6-(4-((2-methyl-3-oxo-1-cyclopentenyl)amino)phenyl)-3-(2H)-pyridazinone;5-methyl-6-{4-[(2-methyl-3-oxocyclopent-1-en-1-yl)amino]phenyl}-4,5-dihydropyridazin-3(2H)-one
Cas No.	125068-54-4
分子式	C₁₇H₁₉N₃O₂
分子量	297.35
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	NSP-805 是一种有效的，选择性的 phosphodiesterase 3 (PDE3) 抑制剂，为一种强心剂，具有舒张血管的作用。

产品详情	NSP-805 是一种有效的，选择性的 phosphodiesterase 3 (PDE3) 抑制剂，为一种强心剂，具有舒张血管的作用。
生物活性	NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3), and a cardiotonic agent with vasodilator properties.
性状	Solid
体外研究(In Vitro)	In isolated guinea pig left atria, NSP-805 shows positive inotropic EC50 value in order of potency of 0.18 μM. The in vitro positive inotropic effects of NSP-805 is accompanied by increases in tissue cyclic AMP and abolished by carbachol. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	In anesthetized dogs, intravenous (i.v.) injection of NSP-805 produces dose-dependent increases in left ventricular VVdp/dtmax and decreases in aortic blood pressure (ABP) with relatively small increases in heart rate (HR). The ED 50 value for LVdP/dtmax of NSP-805 is 12 μg/kg. When the drugs is administered intraduodenally to anesthetized dogs, the ED 50 value for LVdP/dtmax of NSP-805, is approximately 10 μg/kg. In the propranolol-induced heart failure model, NSP-805 completely improves the hemodynamic state of heart failure to normal levels. NSP-805(100 μg/kg) reduces systemic blood pressure significantly, but the increase of chorio-retinal blood flow is less than that at the low dose of NSP-805 (40 μg/kg) in rabbit eyes. has not independently confirmed the accuracy of these methods. They are for
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Mochizuki N, et al. Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties. J Cardiovasc Pharmacol. 1993 Jun;21(6):983-95. [2]. Uchida H, et al. [The effect of phosphodiesterase type 3 inhibitor on chorio-retinal blood flow in rabbits eyes]. Nippon Ganka Gakkai Zasshi. 2002 Oct;106(10):615-20.

溶解度数据	In Vitro: DMSO : 41.67 mg/mL (140.14 mM; Need ultrasonic)配制储备液

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[1]. Mochizuki N, et al. Cardiovascular effects of NSP-804 and NSP-805, novel cardiotonic agents with vasodilator properties. J Cardiovasc Pharmacol. 1993 Jun;21(6):983-95.
[2]. Uchida H, et al. [The effect of phosphodiesterase type 3 inhibitor on chorio-retinal blood flow in rabbits eyes]. Nippon Ganka Gakkai Zasshi. 2002 Oct;106(10):615-20.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

NSP-805

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