在大鼠 HSC（肝星状细胞）和人 HSC 衍生的 TWNT-4 细胞中，盐酸 facsudil (100 μM) 通过阻止细胞扩散、应力纤维产生和 α-SMA 表达来抑制细胞发育[4]。在大鼠 HSC 和人 HSC 衍生的 TWNT-4 细胞中，Fasudil Hydrochronide（50-100 μM；24 小时）可抑制 LPA（溶血磷脂酸）引起的 ERK1/2、JNK 和 p38 磷酸化[4]。在人 HSC 衍生的 TWNT-4 细胞中，facdilin 盐酸盐（25–100 μM；24 小时）可促进 MMP-1 转录，同时抑制胶原蛋白和 TIMP 转录[4]。

在手术前一小时静脉注射时，盐酸法库地尔 (10 mg/kg) 已被证明可以预防心血管疾病，抑制 JNK 激活，并减少缺血期间在线粒体和细胞核之间易位的 AIF 量[5]。盐酸Fasudil (50 mg/kg/d; ip) 抑制蛋白脂质蛋白PLP p139-151，该蛋白可引起急性和复发性实验性自身免疫性脑脊髓炎(EAE)。它还可以减少淋巴细胞增殖，下调白细胞介素 (IL)-17，并显着降低 IFN-γ/IL-4 比率 [6]。 ?Fasudil 盐酸盐（100 mg/kg/d；口服）可抑制小鼠脊髓的炎症、脱髓鞘、轴突损失和 APP 阳性。它还显着降低了SJL/J小鼠实验性自身免疫性脑脊髓炎（EAE）的发生率和病理检查评分[6]。

Western Blot 分析[4]
细胞类型：大鼠 HSC 和人 HSC 衍生的 TWNT-4 细胞
测试浓度： 50 μM； 100 μM
孵育时间： 24 小时
实验结果： 将 LPA 诱导的 ERK1/2、JNK 和 p38 MAPK 磷酸化抑制 60分别为 %、70% 和 90%。

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RT-PCR[4]
细胞类型：大鼠 HSC 和人 HSC 衍生的 TWNT-4 细胞
测试浓度： 25微米； 50μM； 100 μM 24 小时
孵育时间：24 小时
实验结果：降低 I 型胶原蛋白、a-SMA、和TIMP-1。

Animal/Disease Models: Myocardial ischemia and reperfusion in rat (250-300 g)[5]
Doses: 10 mg/kg
Route of Administration: intravenous (iv) injection; 1 h before operation
Experimental Results: Activated the Rho-kinase, JNK, and resulted AIF translocated to the nucleus. Inhibited Rho-kinase activity, and decreased myocardial infarct size and heart cell apoptosis.

[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.
[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.
[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.
[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.
[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.
[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.
[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.

C14H17N3O2S.HCL

327.83

105628-07-7

Fasudil;103745-39-7;Fasudil dihydrochloride;203911-27-7

Cl[H].S(C1=C([H])C([H])=C([H])C2C([H])=NC([H])=C([H])C1=2)(N1C([H])([H])C([H])([H])N([H])C([H])([H])C([H])([H])C1([H])[H])(=O)=O

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (6.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 4: Saline: 30 mg/mL

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Solubility in Formulation 5: 100 mg/mL (305.04 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。