所有图片(1)
别名:
(-)-OR-1259, (R)-Simendan, 2-[2-[4-[(4R)-1,4,5,6-Tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]hydrazinylidene]-propanedinitrile, OR 1259, R)-((4-(1,4,5,6-Tetrahydro-4-methyl-6-oxo-3-pyridazinyl)phenyl)hydrazono) propanedintrile
经验公式（希尔记法）:
C14H12N6O
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质量水平
检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D -500 to -650°, c = 0.5 in THF
颜色
yellow
溶解性
DMSO: ≥20 mg/mL
储存温度
room temp
SMILES字符串
C[C@@H]1CC(=O)NN=C1c2ccc(N\N=C(\C#N)C#N)cc2
InChI
1S/C14H12N6O/c1-9-6-13(21)19-20-14(9)10-2-4-11(5-3-10)17-18-12(7-15)8-16/h2-5,9,17H,6H2,1H3,(H,19,21)/t9-/m1/s1
InChI key
WHXMKTBCFHIYNQ-SECBINFHSA-N
基因信息
human ... PDE3A(5139) , PDE3B(5140) , TNNC1(7134) , TNNI3(7137) , TNNT2(7139)
应用
Levosimendan has been used for screening its anti-human immunodeficiency virus type 1 (HIV-1) property. It has also been used for screening its cytotoxic effects in TP53 mutant and wild-type lung adenocarcinoma cell lines
生化/生理作用
Levosimendan has a potential to inhibit both acute human immunodeficiency virus type 1 (HIV-1) replication and the reactivation of latent HIV-1 proviruses. Therefore, it is considered to be a promising anti-HIV-1 agent.
Levosimendan is a calcium sensitiser. The compound increases the sensitivity of the heart to calcium, thus increasing cardiac contractility without a rise in intracellular calcium. Levosimendan binds to cardiac troponin C in a calcium-dependent manner and stabilizes troponin C. This is followed by actin-myosin cross-bridges, without increasing myocardial consumption of ATP. Additionally the compound acts as vasodilator by opening an ATP-sensitive potassium channels. Levosimendan is a drug used for treatment of congestive heart failure. Also it can be used to treat calcium channel blocker overdose.
警示用语：
Warning
危险分类
Acute Tox. 4 Dermal - Acute Tox. 4 Inhalation - Acute Tox. 4 Oral
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Screening of an FDA-approved compound library identifies levosimendan as a novel anti-HIV-1 agent that inhibits viral transcription
Hayashi T, et al.
Antiviral research, 146, 76-85 (2017)
Chih-Hung Wang et al.
Journal of the American Heart Association, 9(12), e016139-e016139 (2020-06-02)
Background This study investigated whether levosimendan, an inotropic calcium sensitizer, when combined with moderate therapeutic hypothermia, may exert synergistic benefits on post-cardiac arrest myocardial dysfunction and improve outcomes. Methods and Results After 9.5-minute asphyxia-induced cardiac arrest and resuscitation, 48 rats
Brittney A Klein et al.
Biochemistry, 57(15), 2256-2265 (2018-03-21)
The development of calcium sensitizers for the treatment of systolic heart failure presents difficulties, including judging the optimal efficacy and the specificity to target cardiac muscle. The thin filament is an attractive target because cardiac troponin C (cTnC) is the
Julia Hasslacher et al.
Critical care (London, England), 15(4), R166-R166 (2011-07-14)
Levosimendan is an extensively investigated inodilator showing also cardioprotective and antiinflammatory effects. The aim of our study was to explore the influence of levosimendan on polymorphonuclear leucocytes (PMN), a main source of reactive oxygen species, in vitro and in patients
A Candidate Cell-Selective Anticancer Agent
Probe Reports from the NIH Molecular Libraries Program, 146, 76-85 (2014)
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