Fasudil (HA-1077) HCl|105628-07-7|(盐酸法舒地尔; HA-1077 Hydrochloride; AT-877 Hydrochloride)-陌孚医药/Medlife

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Fasudil (HA-1077) HCl (Synonyms: 盐酸法舒地尔; HA-1077 Hydrochloride; AT-877 Hydrochloride)

目录号: PC15939 纯度: ≥98%

CAS No. :105628-07-7

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中文名称	Fasudil (HA-1077) HCl
中文别名	盐酸法舒地尔;六氢-1-(5-异喹啉磺酰基)-1H-1,4-二氮杂卓盐酸盐;Fasudil Hydrochloride 盐酸法舒地尔;Fasudil hydrochloride 抑制剂;盐酸法苏地尔;(5-异喹啉磺酰基)高哌嗪盐酸盐;5-(1-高哌嗪)磺酰基异喹啉盐酸盐
英文名称	Fasudil (HA-1077) HCl
英文别名	1-(5-ISOQUINOLINESULFONYL)-1H-HEXAHYDRO-1,4-DIAZEPINE, DIHYDROCHLORIDE;1-(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE 2HCL;1-(5-ISOQUINOLINESULFONYL)-HOMOPIPERAZINE DIHYDROCHLORIDE;1-(5-ISOQUINOLINESULFONYL)-HOMOPIPERAZINE HCL;1-(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE HYDROCHLORIDE;1-(5-ISOQUINOLINYLSULFONYL)HOMOPIPERAZINE DIHYDROCHLORIDE;5-(1,4-DIAZEPAN-1-YLSULFONYL)ISOQUINOLINE HYDROCHLORIDE;(5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE, 2HCL;FASUDEL;FASUDIL DIHYDROCHLORIDE;FASUDIL HCL;FASUDIL HYDROCHLORIDE;HA-1077;HA-1077 DIHYDROCHLORIDE;HEXAHYDRO-1-(5-ISOQUINOLINYLSULFONYL)-MONOHYDROCHLORIDE;Fasudil Monohydrochloride Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine monohydrochloride;4-Methoxyphenylacetic acid;5-((1,4-Diazepan-1-yl)sulfonyl)isoquinoline hydrochloride;FASUDIL;Fasudil (HA-1077) HCl;Fasudil (Hydrochloride);Fasudil Monohydrochloride;5-(1-Homopiperazinyl)sulfonylisoquinoline Hydrochloride;AT-877;Hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine monohydrochloride;Eril;AT 877 hydrochloride;HA 1077 hydrochloride;SQ04N8S7BR;DSSTox_RID_81004;DSSTox_CID_25615;DSSTox_GSID_45615;C14H18ClN3O2S;1H-1,;C14H17N3O2S.HCl;1H-1,4-Diazepine, hexahydro-1-(5-isoquinolinylsulfonyl)-, monohydrochloride
Cas No.	105628-07-7
分子式	C₁₄H₁₈ClN₃O₂S
分子量	327.83
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

Fasudil (HA-1077; AT877) Hydrochloride is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i of 0.33 μM for ROCK1, IC₅₀s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil Hydrochloride is also a potent Ca channel antagonist and vasodilator.

性状

Solid

IC50 & Target[1][2]

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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Myocardial ischemia and reperfusion in rat (250-300 g)
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.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

参考文献

[1]. Chen M, et al. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22(4):537-50. [Information]

[2]. Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239(1-2):61-7. [Information]

[3]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. [Information]

[4]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38. [Information]

[5]. Corbin KD, et al. Choline metabolism provides novel insights into nonalcoholic fatty liver disease and its progression. Curr Opin Gastroenterol. 2012 Mar;28(2):159-65. [Information]

[6]. Zhang J, 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. [Information]

[7]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. Epub 2006 Sep 22. [Information]

溶解度数据

体外研究:

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

DMSO : ≥ 31 mg/mL (94.56 mM)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.0504 mL	15.2518 mL	30.5036 mL
5 mM	0.6101 mL	3.0504 mL	6.1007 mL
10 mM	0.3050 mL	1.5252 mL	3.0504 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (305.04 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 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 ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 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.

建议依照次序添加每种溶剂： 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。

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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