Fasudil hydrochloride - CAS 105628-07-7
Catalog number:
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
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
Publictions citing BOC Sciences Products
  • >> More
White Crystalline Solid
Fasudil hydrochloride; Fasudil HCl; Eril; Fasudil (Hydrochloride); Fasudil Monohydrochloride; AT-877; HA-1077
DMSO: 5 mg/mL Water: 65 mg/mL
-20ºC Freeze
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
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related ROCK Products

SAR-407899 hydrochloride
(CAS: 923262-96-8)

SAR-407899 hydrochloride is the hydrochloride form of SAR-407899, which is a potent, ATP-competitive ROCK inhibitor. It has good antihypertensive activity.

CAS 105628-07-7 Fasudil hydrochloride

Fasudil hydrochloride
(CAS: 105628-07-7)

Fasudil HCl, a 5-isoquinolinesulfonamide derivative, is a highly selective Rho-associated protein kinase inhibitor that might have a rate in romoting the recove...

CAS 850664-21-0 GSK 269962

GSK 269962
(CAS: 850664-21-0)

GSK 269962 is a potent ROCK inhibitor with IC50 values are 1.6 and 4 nM for recombinant human ROCK1 and ROCK2 respectively, which displays greater than 30-fold ...

CAS 864082-47-3 GSK429286A

(CAS: 864082-47-3)

GSK429286A is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.

(CAS: 923359-38-0)

SAR-407899 is a potent, ATP-competitive ROCK inhibitor. It is equipotent against human and rat-derived Rho-kinase 2 with inhibition constant values of 36 nM and...

CAS 155558-32-0 Hydroxyfasudil Hydrochloride

Hydroxyfasudil Hydrochloride
(CAS: 155558-32-0)

Hydroxyfasudil Hydrochloride, an active metabolite of Fasudil, preferentially inhibits Rho-kinase and plays a central role in the pathogenesis of coronary arter...

CAS 146986-50-7 Y27632 2HCL

Y27632 2HCL
(CAS: 146986-50-7)

CAS 911417-87-3 KD025 (SLx-2119)

KD025 (SLx-2119)
(CAS: 911417-87-3)

KD025 is an orally available, and selective ROCK2 inhibitor with IC50 and Ki of 60 nM and 41 nm, respectively. Phase 2.

CAS 1273579-40-0 Chroman 1

Chroman 1
(CAS: 1273579-40-0)

Chroman 1, a chroman-based compound, is an effective ROCK II inhibitor which could probably influence the cell motility involved in sorts of disorders.

CAS 557782-81-7 ZINC00881524

(CAS: 557782-81-7)

ZINC00881524 is a specific ROCK inhibitor.

CAS 129830-38-2 Y-27632 2HCl

Y-27632 2HCl
(CAS: 129830-38-2)

Y-27632 2HCl inhibits ROCK-II while displaying little activity against PKC, cAMP-dependent protein kinase and myosin light-chain kinase (MLCK) with Ki of 26 μM,...

(CAS: 817194-38-0)

GSK180736A is a selective GRK2 inhibitor with an IC50 of 0.77 μM. It is also a weak inhibitor of PKA with an IC50 of 30 μM, but highly potent against ROCK1 (IC5...

Netarsudil Mesylate
(CAS: 1422144-42-0)

CAS 451462-58-1 (S)-H-1152 dihydrochloride

(S)-H-1152 dihydrochloride
(CAS: 451462-58-1)

(S)-H-1152 dihydrochloride is a Rho-kinase inhibitor and cell permeable inhibitor of ROCK (Ki = 1.6 nM).

CAS 1072959-67-1 N-[2-[2-(Dimethylamino)ethoxy]-4-(1H-pyrazol-4-yl)phenyl]-2,3-dihydro-1,4-benzodioxin-2-carboxamide

(CAS: 1072959-67-1)

SR 3677 is an effective ROCK inhibitor, espectially against ROCK II and it could block the phosphorylation ofmyosin light chain and promote the outflow of aqueo...

(CAS: 1414854-42-4)

Verosudil is a selective Rho-kinase inhibitor originated by Aerie Pharmaceuticals. In Jun 2013, Phase-II for Ocular hypertension in USA was discontinued. In Sep...

CAS 1226056-71-8 Thiazovivin

(CAS: 1226056-71-8)

CAS 105628-72-6 Hydroxyfasudil

(CAS: 105628-72-6)

Hydroxyfasudil, formed through the metabolism action of Fasudil, could be useful in improving the symptoms of pulmonary hypertension for playing the role as an ...

CAS 867017-68-3 6-Chloro-n4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine

(CAS: 867017-68-3)

6-Chloro-n4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine is potent and highly selective ROCK inhibitor. Its IC50 v...

CAS 199433-58-4 Y-33075

(CAS: 199433-58-4)

Y-33075, also called as SNJ-1656, a well-characterized ROCK inhibitor, inhibits more potently ROCK by about 30 times than Y-27632, a common specific ROCK inhibi...

Chemical Structure

CAS 105628-07-7 Fasudil hydrochloride

Quick Inquiry

Verification code

Featured Items