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名称

NSP-805

英文别名

4,5-Dihydro-5-methyl-6-(4-((2-methyl-3-oxo-1-cyclopentenyl)amino)phenyl)-3-(2H)-pyridazinone | F81718 | 3-[4-(6-Hydroxy-4-methyl-4,5-dihydropyridazin-3-yl)anilino]-2-methylcyclopent-2-en-1-one | MS-24267 | Nsp 805 | 4,5-Dihydro-6-(4-((2-methyl-3-oxo-1-cyc

英文名称

NSP-805

货号

N648202-5mg

包装规格

5mg

浓度

≥99%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

NSP-805 is a potent and selective inhibitor of guinea pig cardiac phosphodiesterase 3 (PDE3) , and a cardiotonic agent with vasodilator properties. In Vitro In isolated guinea pig left atria, NSP-805 shows positive inotropic EC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid

生化机理

NSP-805 是一种强效的豚鼠心脏磷酸二酯酶 3 (PDE3) 选择性抑制剂，也是一种具有血管扩张特性的强心剂。

CAS号

125068-54-4

分子式

C17H19N3O2

分子量

297.35 g/mol

PubChem编号

130349

Isomeric SMILES

CC1CC(=O)NN=C1C2=CC=C(C=C2)NC3=C(C(=O)CC3)C

IIUPAC Name

4-methyl-3-[4-[(2-methyl-3-oxocyclopenten-1-yl)amino]phenyl]-4,5-dihydro-1H-pyridazin-6-one

INCHI

1S/C17H19N3O2/c1-10-9-16(22)19-20-17(10)12-3-5-13(6-4-12)18-14-7-8-15(21)11(14)2/h3-6,10,18H,7-9H2,1-2H3,(H,19,22)

InChi Key

DSRIICXPBQXOKK-UHFFFAOYSA-N

Smiles

CC1CC(=O)NN=C1C2=CC=C(C=C2)NC3=C(C(=O)CC3)C

PubChem CID

130349

关联CAS

125068-54-4

MeSH Entry Terms

4,5-dihydro-5-methyl-6-(4-((2-methyl-3-oxo-1-cyclopentenyl)amino)phenyl)-3-(2H)-pyridazinone;NSP 805;NSP-805

溶解性

DMSO : 41.67 mg/mL (140.14 mM; Need ultrasonic)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

297.148 Da

单同位素质量Monoisotopic Mass

297.148 Da

拓扑极表面积Topological Polar Surface Area

70.600 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

542

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

1.7

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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