Fasudil hydrochloride - CAS 105628-07-7
Catalog number:
105628-07-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C14H18ClN3O2S
Molecular Weight:
327.83
COA:
Inquire
Targets:
ROCK
Description:
Fasudil HCl, a 5-isoquinolinesulfonamide derivative, is a highly selective Rho-associated protein kinase inhibitor that might have a rate in romoting the recovery of neurological function, reducing clinical symptoms and the morbidity. IC50: 0.74μM. It was
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Purity:
>98%
Appearance:
White Crystalline Solid
Synonyms:
Fasudil hydrochloride; Fasudil HCl; Eril; Fasudil (Hydrochloride); Fasudil Monohydrochloride; AT-877; HA-1077
Solubility:
DMSO: 5 mg/mL Water: 65 mg/mL
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
Fasudil HCl, a 5-isoquinolinesulfonamide derivative, is a highly selective Rho-associated protein kinase inhibitor that might have a rate in romoting the recovery of neurological function, reducing clinical symptoms and the morbidity.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Grams-Kilos
Density:
1.289g/cm3
InChIKey:
NGOGFTYYXHNFQH-UHFFFAOYSA-N
InChI:
InChI=1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14/h1,3-5,7,11,15H,2,6,8-10H2
Canonical SMILES:
C1CNCCN(C1)S(=O)(=O)C2=CC=CC3=C2C=CN=C3
1.HA1077, a protein kinase inhibitor, inhibits calponin phosphorylation on Ser175 in porcine coronary artery.
Nagumo H1, Seto M, Sakurada K, Walsh MP, Sasaki Y. Eur J Pharmacol. 1998 Nov 6;360(2-3):257-64.
Calponin is a thin filament-associated protein which has been implicated in the modulation of the contractile state of smooth muscle via its interaction with actin and inhibition of the actin-activated myosin Mg-ATPase. This inhibitory effect is alleviated by phosphorylation of calponin at Ser175 in vitro by protein kinase C. The issue of calponin phosphorylation in intact smooth muscle in response to agonists that activate protein kinase C is controversial. We have produced a monoclonal antibody that specifically recognizes calponin phosphorylated at Ser175 and used it to analyze calponin phosphorylation in porcine coronary arterial smooth muscle stimulated with prostaglandin F2alpha or phorbol 12,13-dibutylate (PDB). Calponin phosphorylation increased rapidly in response to prostaglandin F2alpha concomitant with the increase in tension. Calponin was then dephosphorylated while force was maintained. Tension development in response to PDB was significantly slower, but again calponin phosphorylation paralleled force development.
2.Inhibition by the protein kinase inhibitor HA1077 of the activation of NADPH oxidase in human neutrophils.
Arai M1, Sasaki Y, Nozawa R. Biochem Pharmacol. 1993 Oct 19;46(8):1487-90.
The effect of an inhibitor of protein kinase, HA1077 [1-(5-isoquinolinesulfonyl)-homopiperazine HCl], and its hydroxylated metabolite, HA1100, on the activation of NADPH oxidase in human neutrophils were studied. Cells were preincubated with each drug for 10 min and then activated by treatment with phorbol myristate acetate (PMA) or formylmethionyl leucyl phenylalanine (FMLP). After activation, the rate of superoxide dismutase-inhibitable reduction of cytochrome c was estimated. HA1077 and HA1100 inhibited the PMA-induced production of O2- by neutrophil NADPH oxidase in a concentration-dependent manner (IC50 = 15 and 24 microM, respectively). The sensitivity of the FMLP-induced production of O2- to these drugs was similar. The production of O2- in 1,25-dihydroxyvitamin D3-treated HL-60 cells, which differentiated to macrophage-like cells, was also inhibited by the drugs. The extent of inhibition by HA1077 was almost the same as that by a calmodulin inhibitor (W-7) and by inhibitors of protein kinase (H-7 and H-8).
3.Neuroprotection against cerebral ischemia/reperfusion injury by intravenous administration of liposomal fasudil.
Fukuta T1, Asai T2, Sato A2, Namba M2, Yanagida Y2, Kikuchi T2, Koide H2, Shimizu K2, Oku N3. Int J Pharm. 2016 Apr 20;506(1-2):129-137. doi: 10.1016/j.ijpharm.2016.04.046. [Epub ahead of print]
Fasudil, a Rho-kinase inhibitor, is a promising neuroprotectant against ischemic stroke; however, its low bioavailability is an obstacle to be overcome. Our previous study revealed that the liposomal drug delivery system is a hopeful strategy to increase the therapeutic efficacy of neuroprotectants. In the present study, the usefulness of intravenously administered liposomal fasudil for cerebral ischemia/reperfusion (I/R) injury treatment was examined in transient middle cerebral artery occlusion (t-MCAO) rats. The results showed that PEGylated liposomes of approximately 100nm in diameter accumulated more extensively in the I/R region compared with those of over 200nm. Confocal images showed that fluorescence-labeled liposomal fasudil was widely distributed in the I/R region, and was not noticeably taken up by microglia, which are well-known resident macrophages in the brain, and neuronal cells. These data indicated that liposomal fasudil mainly exerted its pharmacological activity by releasing fasudil from the liposomes in the I/R region.
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CAS 105628-07-7 Fasudil hydrochloride

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