H139
HA-1077 二盐酸盐
solid, ≥98% (HPLC)
别名:
1-（5-异喹啉磺酰基）高哌嗪 二盐酸盐, 法舒地尔 二盐酸盐
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关于此项目
经验公式（希尔记法）:
C14H17N3O2S · 2HCl
化学文摘社编号:
分子量:
364.29
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
HA-1077 二盐酸盐, solid, ≥98% (HPLC)
InChI
1S/C14H17N3O2S.2ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;;/h1,3-5,7,11,15H,2,6,8-10H2;2*1H
SMILES string
Cl[H].Cl[H].O=S(=O)(N1CCCNCC1)c2cccc3cnccc23
InChI key
NOXXIYDYFSNHDF-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
storage condition
desiccated
color
white to off-white
solubility
H2O: >10 mg/mL
Quality Level
Application
HA-1077 二盐酸盐已被用于：
- 舒张悬臂梁
- 在离体冠状动脉功能评估中的作用
- ，以探讨氮杂吲哚-1、法舒地尔对急性缺氧性肺血管收缩 (HPV)
Biochem/physiol Actions
HA-1077/法舒地尔 是一种 Rho 激酶抑制剂。这种 ROCK 抑制剂能够增加患有阿尔茨海默氏症(AD)的动物的认知缺陷。在人体中，法舒地尔对蛛网膜下腔出血 (SAH) 后脑血管痉挛具有较好的治疗作用。HA-1077 也可作为蛋白激酶的抑制剂，如肌球蛋白轻链激酶和 Rho 相关激酶。因此，它可以阻止肌球蛋白磷酸化。
作为细胞内 Ca2+ 拮抗剂抑制血管平滑肌收缩的新型血管扩张剂。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
M Seto et al.
European journal of pharmacology, 195(2), 267-272 (1991-03-26)
We examined the effects of HA1077, a potent inhibitor of protein kinases in vitro, on the relationship between tension and myosin-light chain (MLC20) phosphorylation in the initial phase of contraction of the rabbit aorta. The dose-response curve of HA1077 for
Fasudil exerts cardioprotection in Animal Models of Myocardial Ischemia/Reperfusion injury: A Meta-analysis and Review of Preclinical Evidence and Possible Mechanisms
Huang Y, et al.
Frontiers in Pharmacology, 9, 1083-1083 (2018)
Leptin augments coronary vasoconstriction and smooth muscle proliferation via a Rho-kinase-dependent pathway
Noblet J N, et al.
Basic Research in Cardiology, 111(3), 25-25 (2016)
M Shirotani et al.
The Journal of pharmacology and experimental therapeutics, 259(2), 738-744 (1991-11-01)
The effects of a newly developed vasodilator agent, HA1077 [1-(5-isoquinolinesulfonyl)-homopiperazine hydrochloride], were investigated on the proliferation of cultured bovine aortic vascular smooth muscle cells (VSMC). HA1077 (10-100 microM) inhibited both fetal calf serum-induced proliferation and [3H]thymidine incorporation into DNA of
T Asano et al.
British journal of pharmacology, 98(4), 1091-1100 (1989-12-01)
The in vitro and in vivo vasorelaxant effects of HA1077, 1-(5-isoquinolinesulphonyl)-homopiperazine HCl, a novel vasodilator were examined. The inhibitory effects of HA1077 on contractile responses to various agonists were examined on strips of rabbit aorta. The concentration-response curves to 5-hydroxytryptamine
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