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货号:A702414 同义名: AT877;HA-1077

Fasudil HCl is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

Fasudil 化学结构 CAS号:103745-39-7
Fasudil 化学结构
CAS号:103745-39-7
Fasudil 3D分子结构
CAS号:103745-39-7
Fasudil 化学结构 CAS号:103745-39-7
Fasudil 3D分子结构 CAS号:103745-39-7
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Fasudil 纯度/质量文件 产品仅供科研

货号:A702414 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PKA 其他靶点 纯度
Daphnetin +

PKA, IC50: 9.33 μM

PKC,EGFR 95%
AT13148 ++++

PKA, IC50: 3 nM

98+%
A-674563 HCl +++

PKA, Ki: 16 nM

99%
H-89 2HCl ++

PKA, Ki: 48 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 PKC PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ 其他靶点 纯度
Daphnetin +

PKC, IC50: 25.01 μM

PKA,EGFR 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, Ki: 41 nM

ROCK2, IC50: 60 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 99%
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 其他靶点 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

99%
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。
产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

99%+
Dronedarone Hydrochloride 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

ERK,p38 MAPK,ROS 99%+
Fasudil HCl PKA,Rho 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 99%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 99%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 99%
NP118809 +

N-type Ca2+ channel, IC50: 0.11 μM

L-type calcium channel, IC50: 12.2 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 99%
Cinepazide Maleate 99% (HPLC)
Terfenadine 98%
YM-58483 99%+
Ranolazine 98%
Praeruptorin A p38 MAPK,Akt 98%
Ranolazine 2HCl 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

98%
Levamlodipine besylate 97%
Carboxyamidotriazole Orotate 98%
IGS-1.76 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 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 Autophagy 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

97%
Hydroxychloroquine sulfate 99%
Valproic acid sodium HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

99%+
ROC-325 99%+
Autophinib +++

Autophagy, IC50: 40 nM

99%
Lys05 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 生物活性

描述 Fasudil hydrochloride is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM, respectively.

Fasudil 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
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 <<
NCT03404843 Cardiovascular Diseases Phase 2 Completed - United States, Colorado ... 展开 >> Colorado State University, Dept. of Health and Exercise Science Fort Collins, Colorado, United States, 80523 收起 <<
NCT01823081 Diabetic Macular Edema Phase 3 Completed - Iran, Islamic Republic of ... 展开 >> Tehran, Iran, Islamic Republic of 收起 <<

Fasudil 参考文献

[1]Zhang J, Li XX, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80.

[2]Ono-Saito N, Niki I, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31.

Fasudil 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.43mL

0.69mL

0.34mL

17.16mL

3.43mL

1.72mL

34.32mL

6.86mL

3.43mL

Fasudil 技术信息

CAS号103745-39-7
分子式C14H17N3O2S
分子量 291.369
别名 AT877;HA-1077
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place,Sealed in dry,Store in freezer, under -20°C

溶解方案
动物实验配方
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