产品名称

英文名称：HA-1077 dihydrochloride

同义词

203911-27-7、Fasudil dihydrochloride、HA-1077 DIHYDROCHLORIDE、5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline dihydrochloride、ha-1077、Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride (12)、Fasudil (dihydrochloride)、5-(1,4-diazepan-1-yl、法舒地尔 二盐酸盐、HA-1077 二盐酸盐、Fasudil 二盐酸

产品性质

CAS编号：203911-27-7

分子式：C14H17N3O2S· 2HCl

分子量：364.29

MDL号：MFCD00153805

PubChem编号：16219471

别名：法舒地尔 二盐酸盐|HA-1077 二盐酸盐|Fasudil 二盐酸

英文别名：203911-27-7|Fasudil dihydrochloride|HA-1077 DIHYDROCHLORIDE|5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline dihydrochloride|ha-1077|Isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-, hydrochloride (12)|Fasudil (dihydrochloride)|5-(1,4-diazepan-1-yl

规格或纯度：98% (HPLC)

英文名称：HA-1077 dihydrochloride

生化机理：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。

储存温度：-20°C储存

运输条件：超低温冰袋运输

产品介绍：HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2.HA-1077 dihydrochloride has been shown to be a vasodilating agent as well as a potent inhibitor of Rock-2 (Rho-associated Kinase II), cGKI (cGMP-dependent protein kinase), PKA (cAMP-dependent protein kinase), MYLK, and CaMKII. Rho kinase signaling pathways are thought to cause invasion, migration, and proliferation of certain cells. Studies have shown this compound can also inhibit myosin light chain kinase in vitro and suppress cell rounding by myosin light chain phosphorylation. Mechanistic experiments report that HA-1077 inhibits vascular smooth muscle contraction by acting as a calcium channel protein inhibitor. HA-1077 dihydrochloride is an inhibitor of MSK1, PKC, PRK2 and Rsk-2.

IUPAC Name：5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;dihydrochloride

INCHI：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

Canonical SMILES：C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl.Cl

Isomeric SMILES：C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl.Cl

WGK Germany：3

RTECS：HM4031166

PubChem CID：16219471

溶解性：Soluble in water (>20 mg/ml), DMSO (~2 mg/ml), methanol, DMF (~2 mg/ml), and PBS, pH 7.2 (~5 mg/ml).

熔点：248-249° C

个人防护装备：Eyeshields， Gloves， type N95 (US)， type P1 (EN143) respirator filter

产品包装