Fasudil hydrochloride

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Cat.No. 0541 - Fasudil hydrochloride | C14H17N3O2S.HCl | CAS No. 105628-07-7
Description: Inhibitor of cyclic nucleotide dependent- and Rho-kinases
Alternative Names: HA 1077
Purity: ≥98% (HPLC)
Datasheet
Citations (10)
Literature

Biological Activity

Cyclic nucleotide-dependent protein kinase inhibitor and Rho-associated kinase inhibitor (IC50 = 10.7 μM). Suppress MMP-2 expression and induce apoptosis in glioblastoma cells in vivo. Ca2+ antagonist and vasodilator. Also inhibits proliferation of vascular smooth muscle cells.

Compound Libraries

Fasudil hydrochloride is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox I. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 327.83
Formula C14H17N3O2S.HCl
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 105628-07-7
PubChem ID 163751
InChI Key LFVPBERIVUNMGV-UHFFFAOYSA-N
Smiles Cl.O=S(=O)(N1CCCNCC1)C1=C2C=CN=CC2=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 32.78 100

Preparing Stock Solutions

The following data is based on the product molecular weight 327.83. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.05 mL 15.25 mL 30.5 mL
5 mM 0.61 mL 3.05 mL 6.1 mL
10 mM 0.31 mL 1.53 mL 3.05 mL
50 mM 0.06 mL 0.31 mL 0.61 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Arai et al (1993) Inhibition by the protein kinase inhibitor HA-1077 of the activation of NADPH oxidase in human neutrophils. Biochem.Pharmacol. 46 1487 PMID: 8240400

Shirotani et al (1991) A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture. J.Pharmacol.Exp.Ther. 259 738 PMID: 1941621

Satoh et al (1996) Neuroprotective properties of a protein kinase inhibitor against ischaemia-induced neuronal damage in rats and gerbils. Br.J.Pharmacol. 118 1592 PMID: 8842419

Sward et al (2000) Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum. J.Physiol. 522 33 PMID: 10618150

Deng et al (2010) Rho-kinase inhibitor, fasudil, suppresses glioblastoma cell line progression in vitro and in vivo. Cancer Biol Ther. 875 875 PMID: 20364104


If you know of a relevant reference for Fasudil hydrochloride, please let us know.

View Related Products by Product Action

View all Rho-Kinases Inhibitors

Keywords: inhibitors inhibits cyclic nucleotide dependent- Rho-kinases HA1077 HA 1077 Rho-kinases

10 Citations for Fasudil hydrochloride

Citations are publications that use Tocris products. Selected citations for Fasudil hydrochloride include:

Jeyaraj et al (2012) Cyclic AMP-Rap1A signaling activates RhoA to induce α(2c)-adrenoceptor translocation to the cell surface of microvascular smooth muscle cells. Br J Pharmacol 303 C499 PMID: 22621783

Wang et al (2012) Inhibition of TNF-α improves the bladder dysfunction that is associated with type 2 diabetes. BMC Ear Nose Throat Disord 61 2134 PMID: 22688336

Díez et al (2010) Statins inhibit angiotensin II/Smad pathway and related vascular fibrosis, by a TGF-β-independent process. PLoS One 5 e14145 PMID: 21152444

Choi et al (2009) Comparison of contractile mechanisms of sphingosylphosphorylcholine and sphingosine-1-phosphate in rabbit coronary artery. Diabetes 82 324 PMID: 19218288

Takehara et al (2008) Rho-associated kinase inhibitor Y-27632 promotes survival of cynomolgus monkey embryonic stem cells. Mol Hum Reprod 14 627 PMID: 18940855

Inan and Büyükafşar (2008) Antiepileptic effects of two Rho-kinase inhibitors, Y-27632 and fasudil, in mice. J Neurosci 155 44 PMID: 18536751

Rodríguez-Vita et al (2005) Endothelin-1, via ETA receptor and independently of transforming growth factor-β, increases the connective tissue growth factor in vascular smooth muscle cells. Cardiovasc Res 97 125 PMID: 15976312

Scherer et al (2005) Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss. Am J Physiol Cell Physiol 5 10 PMID: 16316469

Flavahan and Flavahan (2014) The atypical structure and function of newborn arterial endothelium is mediated by Rho/Rho kinase signaling. Am J Physiol Heart Circ Physiol 307 H628 PMID: 24951756

Akhtar et al (2013) Activation of ErbB2 and Downstream Signalling via Rho Kinases and ERK1/2 Contributes to Diabetes-Induced Vascular Dysfunction. PLoS One 8 e67813 PMID: 23826343


Do you know of a great paper that uses Fasudil hydrochloride from Tocris? If so please let us know.

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