| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| Other Sizes |
|
Purity: ≥98%
Fasudil HCl (formerly known as HA1077; HA 1077; HA-1077), the hydrochloride salt of fasudil, is a potent multikinase inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with the potential to be used for the treatment of cerebral vasospasm. It is also a promising drug candidate for a disease-modifying therapy of amyotrophic lateral sclerosis (ALS). Fasudil inhibits ROCK-II, PKA, PKG, PKC, and MLCKwith Ki of 0.33 μM, 1.6 μM, 1.6 μM, 3.3 μM and 36 μM in cell-free assays, respectively. 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 |
In rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells, facsudil hydrochloride (100 μM) suppresses cell development by blocking cell spreading, stress fiber production, and α-SMA expression[4]. In rat HSCs and human HSC-derived TWNT-4 cells, Fasudil Hydrochloride (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, facdilin hydrochloride (25–100 μM; 24 hours) promotes MMP-1 transcription while suppressing collagen and TIMP transcription[4].
|
|---|---|
| ln Vivo |
When administered intravenously one hour before to surgery, facudil hydrochloride (10 mg/kg) has been shown to protect against cardiovascular disease, inhibit JNK activation, and lessen the amount of AIF that is translocated between the mitochondria and nucleus during ischemia[5]. ?Fasudil hydrochloride (50 mg/kg/d; ip) suppresses the proteolipid protein PLP p139-151, which causes acute and relapsing experimental autoimmune encephalomyelitis (EAE). It also decreases lymphocyte proliferation, downregulates interleukin (IL)-17, and significantly lowers the IFN-γ/IL-4 ratio[6]. ?Fasudil hydrochloride (100 mg/kg/d; po) suppresses inflammation, demyelination, axonal loss, and APP positivity in the mouse spinal cord. It also considerably lowers the incidence and pathological examination score of experimental autoimmune encephalomyelitis (EAE) in SJL/J mice[6].
|
| 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 24 hrs (hours) 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]. 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. |
| Molecular Formula |
C14H17N3O2S.HCL
|
|
|---|---|---|
| Molecular Weight |
327.83
|
|
| CAS # |
105628-07-7
|
|
| Related CAS # |
Fasudil;103745-39-7;Fasudil dihydrochloride;203911-27-7
|
|
| SMILES |
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
|
|
| Synonyms |
|
|
| 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)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
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. 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. View More
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. Solubility in Formulation 4: Saline: 30 mg/mL 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. |
| Preparing Stock Solutions | 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 |
*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.
|
|---|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
