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| 10mg | ||
| 25mg | ||
| 50mg | ||
| 100mg |
Fasudil diHCl, the dihydrochloride salt of Fasudil (HA-1077; AT-877), is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK (Ki = 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively) with vasodilatory effects. It is used as a vasodilator for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. Fasudil is found to be effective for the treatment of pulmonary hypertension.
| ln Vitro |
Fasudil dihydrochloride (100 μM) suppresses cell proliferation in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells by preventing cell spreading, stress fiber production, and α-SMA expression[4]. In rat HSCs and human HSC-derived TWNT-4 cells, dihydrochloride (50-100 μM; 24 hours) suppresses the phosphorylation of ERK1/2, JNK, and p38 caused by LPA (lysophoaphatidic acid)[4]. In human HSC-derived TWNT-4 cells, facudil dihydrochloride (25–100 μM; 24 hours) promotes MMP-1 transcription while suppressing collagen and TIMP transcription[4].
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| ln Vivo |
When administered intravenously one hour prior to surgery, facudil dihydrochloride (10 mg/kg) has been shown to protect against cardiovascular disease, inhibit JNK activation, and lessen the amount of AIF that is translocated from the mitochondria to the nucleus during ischemia[5]. Fasudil dihydrochloride (50 mg/kg/d; ip) inhibits the proliferation of lymphocytes, results in downregulation of interleukin (IL)-17, and a significant decrease in the IFN-γ/IL-4 ratio. It also prevents acute and relapsing EAE (experimental autoimmune encephalomyelitis) caused by the proteolipid protein PLP p139-151 [6]. Fasudil dihydrochloride (100 mg/kg/d; po) decreases inflammation, demyelination, axonal loss, and APP positive in the mouse spinal cord and significantly lowers the incidence and pathological examination score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice [6].
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| Cell Assay |
Western Blot Analysis[4]
Cell Types: Rat HSCs and human HSC -derived TWNT-4 cells Tested Concentrations: 50 μM; 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively. RT- PCR[4] Cell Types: Rat HSCs and human HSC-derived TWNT-4 cells Tested Concentrations: 25 μM; 50 μM; 100 μM Incubation Duration: 24 hrs (hours) Experimental Results: decreased the expression of type I collagen, a-SMA, and TIMP- 1. |
| Animal Protocol |
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. |
| References |
[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]. 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. [6]. 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. |
| Molecular Formula |
C14H17N3O2S.2[HCL]
|
|---|---|
| Molecular Weight |
364.29056
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| CAS # |
203911-27-7
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| Related CAS # |
Fasudil Hydrochloride;105628-07-7;Fasudil;103745-39-7;Fasudil hydrochloride semihydrate;186694-02-0
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| SMILES |
C1=CC2=CN=CC=C2C(=C1)S(=O)(=O)N3CCCNCC3.Cl.Cl
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7451 mL | 13.7253 mL | 27.4507 mL | |
| 5 mM | 0.5490 mL | 2.7451 mL | 5.4901 mL | |
| 10 mM | 0.2745 mL | 1.3725 mL | 2.7451 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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