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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)
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Acute pergolide exposure stiffens engineered valve interstitial cell tissues and reduces contractility in vitro
Capulli A K, et al.
Cardiovascular Pathology : the Official Journal of the Society For Cardiovascular Pathology, 25(4), 316-324 (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
Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension
Dahal B K, et al.
European heart journal. Cardiovascular pharmacotherapy, erj01403-erj02009 (2010)
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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