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盐酸法舒地尔

环状核苷酸依赖性和Rho激酶抑制剂
1篇引用文献 COA COA
    级别和纯度:
  • ≥98%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
F122336-100mg
 100mg 现货 Stock Image
F122336-250mg
 250mg 现货 Stock Image
F122336-500mg
 500mg 现货 Stock Image
F122336-1g
 1g 现货 Stock Image
F122336-5g
 5g 现货 Stock Image
F122336-25g
 25g 期货 Stock Image
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基本描述

别名 盐酸法舒地尔 | 5-(1-高哌嗪)磺酰基异喹啉盐酸盐 | (5-异喹啉磺酰基)高哌嗪盐酸盐
英文别名 5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline hydrochloride | 111GE018 | AKOS015897321 | Fasudil HCl - HA-1077 | FT-0631034 | EN300-7361975 | BCP26351 | s1573 | REGID_for_CID_4917 | 5-(1-Homopiperazi
规格或纯度 ≥98%
英文名称 Fasudil Hydrochloride
生化机理 环状核苷酸依赖性蛋白激酶抑制剂和Rho相关激酶抑制剂（IC50 =10.7μM）。在体内抑制MMP-2表达并诱导胶质母细胞瘤细胞凋亡。Ca2 +拮抗剂和血管扩张剂。还抑制血管平滑肌细胞的增殖。
应用 A selective ROCK inhibitor
储存温度 避光,-20°C储存
运输条件 超低温冰袋运输
产品介绍

Fasudil, Monohydrochloride Salt is a cell-permeable, selective ROCK inhibitor which induces neuroprotection in vitro. Studies sμggest that when acting as a ROCK inhibitor, Fasudil reduces neutrophil transendothelial migration by diminishing cytoskeletal rearrangement of endothelial cells. In addition, Fasudil significantly protects against MeHg-induced axonal degeneration and apoptotic cell death in cultured cortical neurons. Alternate studies show that Fasudil plays an important role in osteoblastic differentiation of stromal cells via increasing the mRNA expression of collagen-I, osteocalcin, and bone morphogenetic protein-2 (BMP-2). Furthermore, noggin, a BMP-2 antagonist can reverse the effects of Fasudil induced mRNA expression of collagen-I and osteocalcin. Upon inhibition of Rho-kinase, Fasudil significantly stimulates FGF-2-induced accumulation of vascular endothelial growth factor (VEGF). Fasudil, Monohydrochloride Salt is an inhibitor of cGKI, MSK1, PKA, PRK2, Rock-2, AMPK, CaMKII, Polycystin-1 and Rsk-1.A selective ROCK inhibitor

Fasudil, Monohydrochloride Salt is a cell-permeable, selective ROCK inhibitor which induces neuroprotection in vitro. Studies suggest that when acting as a ROCK inhibitor, Fasudil reduces neutrophil transendothelial migration by diminishing cytoskeletal rearrangement of endothelial cells. In addition, Fasudil significantly protects against MeHg-induced axonal degeneration and apoptotic cell death in cultured cortical neurons. Alternate studies show that Fasudil plays an important role in osteoblastic differentiation of stromal cells via increasing the mRNA expression of collagen-I, osteocalcin, and bone morphogenetic protein-2 (BMP-2). Furthermore, noggin, a BMP-2 antagonist can reverse the effects of Fasudil induced mRNA expression of collagen-I and osteocalcin. Upon inhibition of Rho-kinase, Fasudil significantly stimulates FGF-2-induced accumulation of vascular endothelial growth factor (VEGF). Fasudil, Monohydrochloride Salt is an inhibitor of cGKI, MSK1, PKA, PRK2, Rock-2, AMPK, CaMKII, Polycystin-1 and Rsk-1.
A selective ROCK inhibitor
纯度 ≥98%

关联靶点（人）

CCR2 Tchem C-C chemokine receptor type 2 (5628 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
HTT Tchem Huntingtin (19182 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
KDM4A Tchem Lysine-specific demethylase 4A (52245 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
EHMT2 Tchem Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 (93046 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TDP1 Tchem Tyrosyl-DNA phosphodiesterase 1 (345557 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
GMNN Tbio Geminin (128009 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ATAD5 Tbio ATPase family AAA domain-containing protein 5 (122566 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
IDH1 Tclin Isocitrate dehydrogenase [NADP] cytoplasmic (40980 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
ROCK2 Tclin Rho-associated protein kinase (137 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
TARDBP Tchem TAR DNA-binding protein 43 (40113 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

关联靶点（其它种属）

Galc Galactocerebrosidase (11 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID
SARS-CoV-2 (38078 活性数据)
活性类型 Relation Activity value Units Action Type 期刊 PubMed Id doi Assay Aladdin ID

作用机制

作用机制 Action Type target ID Target Name Target Type Target Organism Binding Site Name 参考文献

名称和识别符

PubChem SID 504757540
分子类型 小分子
IIUPAC Name 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline;hydrochloride
INCHI 1S/C14H17N3O2S.ClH/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;1H
InChi Key LFVPBERIVUNMGV-UHFFFAOYSA-N
Smiles C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
Isomeric SMILES C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
关联CAS 203911-27-7
分子量 327.83
Reaxy-Rn 5466340
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=5466340&ln=

化学和物理性质

溶解性 溶于water, 最高浓度 (mg/mL): 32.78, 最高浓度(mM): 100；溶于DMSO, 最高浓度 (mg/mL): 24.59, 最高浓度(mM): 75
敏感性 对光线敏感
折光率 1.62
沸点 506.2° C
熔点 222 °C
分子量 327.800 g/mol
XLogP3
氢键供体数Hydrogen Bond Donor Count 2
氢键受体数Hydrogen Bond Acceptor Count 5
可旋转键计数Rotatable Bond Count 2
精确质量Exact Mass 327.081 Da
单同位素质量Monoisotopic Mass 327.081 Da
拓扑极表面积Topological Polar Surface Area 70.700 Ų
重原子数Heavy Atom Count 21
形式电荷Formal Charge 0
复杂度Complexity 421.000
同位素原子数Isotope Atom Count 0
定义的原子立体中心计数Defined Atom Stereocenter Count 0
未定义的原子立体中心计数Undefined Atom Stereocenter Count 0
定义的键立体中心计数Defined Bond Stereocenter Count 0
未定义的键立体中心计数Undefined Bond Stereocenter Count 0
所有立体化学键的总数The total count of all stereochemical bonds 0
共价键合单元计数Covalently-Bonded Unit Count 2

安全和危险性（GHS）

象形图 GHS07
信号词 警告
危险声明

H302: 吞食有害
预防措施声明

P264: 处理后要彻底洗手。

P270: 使用本产品时，请勿进食、饮水或吸烟。

P330: 漱口

P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。

P501: 将内容物/容器处理到。。。
WGK Germany 1
RTECS HM4033500
Merck Index 3942

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找到10个结果

批号(Lot Number) 证书类型 货号
I2130277 分析证书 F122336
J2106184 分析证书 F122336
J2106185 分析证书 F122336
A1710017 分析证书 F122336
I2221378 分析证书 F122336
I2222036 分析证书 F122336
I2222046 分析证书 F122336
I2222047 分析证书 F122336
I2222048 分析证书 F122336
I2222052 分析证书 F122336

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引用文献

1. Chen Wenyuanfeng, Qu Yuan, Liu Yining, Zhang Guorui, Sharhan Hasan M., Zhang Xinzhu, Zhang Kunwu, Cao Baocheng.  (2024)  Effects of fasudil on glial cell activation induced by tooth movement.  Progress in Orthodontics,  25  (1): (1-13).  [PMID:39034361] [10.1186/s40510-024-00518-2]

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