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
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
solid
储存条件
desiccated
颜色
white to off-white
溶解性
H2O: >10 mg/mL
SMILES字符串
Cl[H].Cl[H].O=S(=O)(N1CCCNCC1)c2cccc3cnccc23
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
InChI key
NOXXIYDYFSNHDF-UHFFFAOYSA-N
应用
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)
生化/生理作用
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。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
个人防护装备
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)
Manar Hamed Arafa et al.
Life sciences, 254, 117605-117605 (2020-04-13)
Although chloroquine and diclofenac are not cardiovascular drugs, their chronic administration may trigger cardiotoxicity. We, therefore, evaluated the cardiotoxic impact of diclofenac in chloroquine-treated adjuvant arthritic rats and the protective role of Rho-kinase inhibitors. 90 male rats were equally distributed
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)
The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells
Negoro N, et al.
Biochemical and Biophysical Research Communications, 262(1), 211-215 (1999)
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