计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 2 篇同行评审文献引用。
概述
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
Information
Fasudil (HA-1077, AT-877), a potent and selective inhibitor ofRhokinase, displays less potent inhibiton over PKA, PKG, PKC and MLCK with Ki of 1.6, 1.6, 3.3, and 36 μM in cell-free assays, respectively. Fasudil is also acalcium channelblocker.
In vitro
Fasudil is a class of calcium antagonists. Fasudil produces a competitive inhibition of the Ca2+-induced contraction of the depolarized rabbit aorta. Fasudil is able to inhibit contractile responses to KCl, phenylephnne (PHE) and prostaglandin (PG) F2a. Fasudil also exhibits vasodilator actions by inhibition of 5-hydroxytryptamine, noradrenaline, histamine, angiotensin, and dopamine induced spiral strips contraction. Fasudil induces disorganization of actin stress fiber and cell migration inhibition. Fasudil inhibits hepatic stellate cells spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth, but does not induce apoptosis. Fasudil suppresses the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK.
In vivo
Intra-coronary injection of Fasudil to dogs (30 μg i.a.) produces an approximate 50% increase in CBF. Fasudil (0.01, 0.03, 0.1 and 0.3 mg/kg, bolus, i.v.) dose-dependently decreases MBP and increases HR, VBF, CBF, RBF, and FBF. A total dose of 1.0 ng/mL Fasudil increases cardiac output. The infusion of Fasudil i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without significant changes in right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil administration displays protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. The oral administration of Fasudil (a dosage of 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Treatment of mice with Fasudil suppresses the proliferative response of splenocytes to the antigen. Oral administration of Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice.
Cell Data
cell lines：KB3-1, KBV-1, Hela, and Hs578T cells
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
AT-877 | 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline hydrochloride
规格或纯度
10mM in DMSO
英文名称
Fasudil (HA-1077) HCl
生化机理
Fasudil（HA-1077，AT-877）是一种强效的 Rho 激酶选择性抑制剂，对 PKA、PKG、PKC 和 MLCK 的抑制作用较弱，在无细胞实验中的 Ki 值分别为 1.6、1.6、3.3 和 36 μM。Fasudil 还是一种钙通道阻滞剂。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
EC号
805-833-0
分子类型
小分子
Isomeric SMILES
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3.Cl
关联CAS
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=
技术文档
高级数据
化学和物理性质
溶解性
Solubility (25°C) In vitro Water: 48 mg/mL (198.57 mM); DMSO: Insoluble; Ethanol: Insoluble;
折光率
1.62
沸点
506.2° C
熔点
222 °C
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
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+P317: 如果被吞咽：请寻求医疗帮助。
WGK Germany
1
RTECS
HM4033500
Merck Index
3942
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 B2314012 |
分析证书 | F409290 |
技术文档和文章
此产品的引用文献
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 105628-07-7，分子式为 C14H18ClN3O2S，分子量为 327.83 g/mol。
如何获取批次专用COA？
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