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Fasudil hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fasudil hydrochloride图片
CAS NO:105628-07-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
200mg电议
500mg电议
1 g电议
5 g电议

产品名称
盐酸法舒地尔
HA-1077 hydrochloride
AT-877 Hydrochloride
产品介绍
Fasudil (HA-1077; AT877) Hydrochloride 是一种非特异性RhoA/ROCK抑制剂,并抑制蛋白激酶。Fasudil Hydrochloride 抑制ROCK1Ki为 0.33 μM,抑制ROCK2PKAPKCPKGIC50分别为 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil Hydrochloride 也是一种有效的 Ca2+通道拮抗剂和血管扩张剂。
生物活性

Fasudil (HA-1077; AT877) Hydrochloride is a nonspecificRhoA/ROCKinhibitor and also has inhibitory effect on protein kinases, with anKiof 0.33 μM forROCK1,IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM forROCK2andPKA,PKC,PKG, respectively. Fasudil Hydrochloride is also a potent Ca2+channel antagonist and vasodilator[1][2][3].

IC50& Target[1]

p160ROCK

0.33 μM (Ki)

ROCK2

0.158 μM (IC50)

PKA

4.58 μM (IC50)

PKC

12.30 μM (IC50)

PKG

1.65 μM (IC50)

体外研究
(In Vitro)

Fasudil Hydrochloride (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4].
Fasudil Hydrochloride (50-100 μM; 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4].
Fasudil Hydrochloride (25-100 μM; 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4].

Western Blot Analysis[4]

Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:50 μM; 100 μM
Incubation Time:24 hours
Result:Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively.

RT-PCR[4]

Cell Line:Rat HSCs and human HSC-derived TWNT-4 cells
Concentration:25 μM; 50 μM; 100 μM 24 hours
Incubation Time:24 hours
Result:Reduced the expression of type I collagen, a-SMA, and TIMP-1.
体内研究
(In Vivo)

Fasudil Hydrochloride (10 mg/kg; i.v.; 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[5].
Fasudil Hydrochloride (50 mg/kg/d; i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio[6].
Fasudil Hydrochloride (100 mg/kg/d; p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice[6].

Animal Model:Myocardial ischemia and reperfusion in rat (250-300 g)[5]
Dosage:10 mg/kg
Administration:Intravenous injection; 1 h before operation
Result:Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus.
Inhibited Rho-kinase activity, and reduced myocardial infarct size and heart cell apoptosis.
Clinical Trial
分子量

327.83

性状

Solid

Formula

C14H18ClN3O2S

CAS 号

105628-07-7

中文名称

盐酸法舒地尔

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : 55 mg/mL(167.77 mM;Need ultrasonic)

DMSO : ≥ 31 mg/mL(94.56 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0504 mL15.2518 mL30.5036 mL
5 mM0.6101 mL3.0504 mL6.1007 mL
10 mM0.3050 mL1.5252 mL3.0504 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (305.04 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.34 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (6.34 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.34 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。