Fasudil HCl | HA-1077 Hydrochloride;AT-877 Hydrochloride;Fasudil HCl | Other Compounds | PKC | ROCK | TGF-beta/Smad | MLCK | PKG

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盐酸法舒地尔 /Fasudil HCl {[allProObj[0].p_purity_real_show]}

货号：A193859 同义名： HA-1077 Hydrochloride;AT-877 Hydrochloride

Fasudil HCl (HA-1077; AT877)是一种非特异性RhoA/ROCK抑制剂，同时抑制蛋白激酶，对ROCK1的Ki为0.33 μM，对ROCK2、PKA、PKC和PKG的IC50值分别为0.158 μM、4.58 μM、12.30 μM和1.650 μM。Fasudil盐酸盐还是一种强效的Ca2+通道拮抗剂和血管扩张剂。

Fasudil HCl 化学结构
CAS号：105628-07-7

Fasudil HCl 3D分子结构
CAS号：105628-07-7

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Fasudil HCl 纯度/质量文件产品仅供科研

货号：A193859 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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PKC 亚型比较
ROCK 亚型比较
转化生长因子-β 亚型比较

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									EGFR,PKA	95%
Dequalinium Chloride											99%+
Quercetin	✔									Sirtuin,Src	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 μM			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	ROCK ↓ ↑	ROCK1 ↓ ↑	ROCK2 ↓ ↑	其他靶点	纯度
Thiazovivin	+ ROCK, IC50: ~0.5 μM				98%
Netarsudil hydrochloride	++++ ROCK, Ki: 2 nM				99%+
Y-33075 2HCl	++++ ROCK, IC50: 3.6 nM				99%+
ROCK1-IN-1	++ ROCK, Ki: 17nM				95%
GSK429286A		+++ ROCK1, IC50: 14 nM	++ ROCK2, IC50: 63 nM		99%+
Ripasudil		++ ROCK1, IC50: 51 nM	++ ROCK2, IC50: 19 nM		99%+
Belumosudil			++ ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM		99%+
Y-27632 dihydrochloride		++ ROCK1, Ki: 140 nM	+ ROCK2, Ki: 300 nM		99%+
Fasudil HCl			+ ROCK2, Ki: 330 nM	PKG,Rho	98%
Chroman 1		++++ ROCK1, IC50: 52 pM	++++ ROCK2, IC50: 1 pM		99%
BAY-549		++++ ROCK1, IC50: 0.6 nM	++++ ROCK2, IC50: 1.1 nM		99%+
AT13148		+++ ROCK1, IC50: 6 nM	+++ ROCK2, IC50: 4 nM	PKA	98+%
RKI-1447		+++ ROCK1, IC50: 14.5 nM	+++ ROCK2, IC50: 6.2 nM		99%+
Hydroxyfasudil HCl		+ ROCK1, IC50: 0.73 μM	+ ROCK2, IC50: 0.72 μM	PKA	98%
H-1152 2HCl			+++ ROCK2, IC50: 0.0120 μM	PKG	99%
GSK269962A HCl		++++ ROCK1, IC50: 1.6 nM	+++ ROCK2, IC50: 4 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Fasudil HCl 生物活性

靶点

ROCK2

ROCK2, Ki:330 nM
Calcium Channel

描述

Fasudil Hydrochloride is the hydrochloride form of Fasudil with higher solubility. Fasudil is a selective Rock inhibitor with Ki value of 0.33μM, as well as showed inhibitory activity against Protein kinase A, Protein kinase G, Protein kinase C, MLCK with Ki values of 1.6μM, 1.6μM, 3.3μM and 36μM. Addition of 0.3-100μM Fasudil could dose-dependently inhibited Ca²⁺ sensitization of force in guinea-pig ileum. Treatment with fasudil significantly suppressed LCc-EC migration, which may due to its impaction on polymerization of the cytoskeletal actin filament network. Incubation with Fasudil at concentration ranging in 1-100μM in MDA-MB-231 cell colonies for 21 days could concentration-dependently inhibit the the anchorage-independent cell growth in a soft agar assay. In an orthotopic MDA-MB-231 rat model, fasudil did not suppress growth of established tumors, but could greatly reduce the incidence of tumor formation through oral administration at dose of 200 mg/kg/day or continuously in the drink at dose of ~228 mg/kg/day.

Fasudil HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HEK293 cells		Function assay		Inhibition of His-tagged human PRK2 expressed in HEK293 cells, IC50=4 μM.	10998351
insect cells		Function assay	10 mins	Inhibition of human leukocytic ROCK1 expressed in insect cells using KKRNRTLSV as substrate after 10 mins by pyruvate kinase/lactate dehydrogenase coupled assay, Ki=0.53 μM.	26039570
Sf9 cells		Function assay	90 mins	Inhibition of human recombinant N-terminal his-tagged ROCK1 (3-543) expressed in baculovirus infected Sf9 cells using Biotin-Ahx-AKRRLSSLRA-CONH2 substrate and [gamma-33P]ATP after 90 mins by scintillation proximity assay, IC50=0.3 μM.	17018693
Sf9 cells		Function assay		Inhibition of rat ROCK2 expressed in Sf9 cells, IC50=1.9 μM.	10998351

Fasudil HCl 动物研究

Dose	Rat: 30 mg/kg^[3] (i.v.), 10 mg/kg^[4] (i.p.) Mice: 100 mg/kg^[3] (p.o.), 50 mg/kg^[5] (i.p.)
Administration	i.v., p.o., i.p.

Fasudil HCl 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01823081	Diabetic Macular Edema	Phase 3	Completed	-	Iran, Islamic Republic of ... 展开 >> Tehran, Iran, Islamic Republic of 收起 <<
NCT00120718	Atherosclerosis ... 展开 >> Hypercholesterolemia 收起 <<	Phase 2	Completed	-	United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 收起 <<
NCT01069042	Heart Failure	Phase 4	Unknown	November 2010	Taiwan ... 展开 >> National Cheng Kung University Hospital Recruiting Tainan, Taiwan, 70401 Contact: Ping-Yen Liu, MD, PhD 收起 <<

Fasudil HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.05mL

0.61mL

0.31mL

15.25mL

3.05mL

1.53mL

30.50mL

6.10mL

3.05mL

Fasudil HCl 技术信息

CAS号	105628-07-7
分子式	C₁₄H₁₈ClN₃O₂S
分子量	327.83

别名	HA-1077 Hydrochloride;AT-877 Hydrochloride;Fasudil HCl
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 30 mg/mL(91.51 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H₂O: 55 mg/mL(167.77 mM)，配合低频超声助溶

动物实验配方

PO 0.5% CMC-Na 60 mg/mL clear

盐酸法舒地尔 /Fasudil HCl {[allProObj[0].p_purity_real_show]}

Fasudil HCl 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Fasudil HCl 质控信息

Fasudil HCl 生物活性

Fasudil HCl 细胞研究

Fasudil HCl 动物研究

Fasudil HCl 临床研究

Fasudil HCl 实验方案

Fasudil HCl 技术信息

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ROCK2	ROCK2, Ki:330 nM
Calcium Channel

盐酸法舒地尔 /Fasudil HCl {[allProObj[0].p_purity_real_show]}

Fasudil HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Fasudil HCl 质控信息

Fasudil HCl 生物活性

Fasudil HCl 细胞研究

Fasudil HCl 动物研究

Fasudil HCl 临床研究

Fasudil HCl 实验方案

Fasudil HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Fasudil HCl 纯度/质量文件产品仅供科研