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Merck

H139

Sigma-Aldrich

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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About This Item

经验公式(希尔记法):
C14H17N3O2S · 2HCl
分子量:
364.29
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

solid

儲存條件

desiccated

顏色

white to off-white

溶解度

H2O: >10 mg/mL

SMILES 字串

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 密鑰

NOXXIYDYFSNHDF-UHFFFAOYSA-N

應用

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。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

Eyeshields, Gloves, type N95 (US)


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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
Protective effects of the ROCK inhibitor fasudil against cognitive dysfunction following status epilepticus in male rats
Song X, et al.
Journal of Neuroscience Research (2018)
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)
Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension
Dahal B K, et al.
European heart journal. Cardiovascular pharmacotherapy, erj01403-erj02009 (2010)
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

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