Size | Price | Stock | Qty |
---|---|---|---|
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
Fasudil (also known as HA-1077) is a potent inhibitor of ROCK-II, PKA, PKG, PKC, and MLCK with 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, facudil (100 μM) suppresses cell development by blocking cell spreading, stress fiber formation, and α-SMA expression[4]. In rat HSCs and human HSC-derived TWNT-4 cells, facudil (50–100 μM; 24 hours) suppresses the phosphorylation of ERK1/2, JNK, and p38 caused by LPA (lysophoaphatidic acid)[4]. 24-hour exposure to -100 μM) inhibits collagen and TIMP transcription while promoting MMP-1 transcription in human HSC-derived TWNT-4 cells[4].
|
---|---|
ln Vivo |
Fasudil (10 mg/kg; intravenously; one hour prior to surgery) has been shown to protect against cardiovascular disease, lower JNK activation, and lessen AIF's mitochondrial-nuclear translocation during ischemia injury[5]. Fasudil (50 mg/kg/d; ip) inhibits the proliferation of lymphocytes, downregulates the expression of interleukin (IL)-17, and significantly lowers the ratio of IFN-γ to IL-4. It also prevents acute and relapsing EAE (experimental autoimmune encephalomyelitis) caused by the proteolipid protein PLP p139–151[6]. Fasudil (100 mg/kg/d; po) decreases inflammation, demyelination, axonal loss, and APP positive in the mouse spinal cord. It also significantly 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 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
|
|
---|---|---|
Molecular Weight |
291.37
|
|
CAS # |
103745-39-7
|
|
Related CAS # |
Fasudil Hydrochloride;105628-07-7;Fasudil hydrochloride semihydrate;186694-02-0;Fasudil dihydrochloride;203911-27-7
|
|
SMILES |
Cl[H].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) |
|
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4321 mL | 17.1603 mL | 34.3206 mL | |
5 mM | 0.6864 mL | 3.4321 mL | 6.8641 mL | |
10 mM | 0.3432 mL | 1.7160 mL | 3.4321 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.