HA-1077; AT877 MedChemExpress (MCE)

Product Name	Fasudil
Synonyms	at877 Fasudil 103745-39-7 Fasudil HCI Fasudil Hydrchloride Fasudil Hydrochloride Injection (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE Synonyms at877 Fasudil 103745-39-7 Fasudil HCI Fasudil Hydrchloride Fasudil Hydrochloride Injection (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE 1-(5-Isoquinolinesulphonyl)homopiperazine 5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline 1-(5-Isoquinolinylsulfonyl)homopiperazine 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE 5-(1,4-diazepan-4-ium-1-ylsulfonyl)isoquinoline N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine 5-(AZEPAN-4-YLSULFONYL)ISOQUINOLINE DIHYDROCHLORIDE hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline dihydrochloride isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]-
CAS	103745-39-7
EINECS	816-154-4
Chemical Formula	C14H17N3O2S
Molecular Weight	291.37
inchi	InChI=1/C14H17N3O2S.2ClH/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;2*1H
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Descriptions	Fasudil Fasudil MedChemExpress (MCE) HY-10341A 103745-39-7 HA-1077 Descriptions Fasudil Fasudil MedChemExpress (MCE) HY-10341A 103745-39-7 HA-1077 AT877 Please store the product under the recommended conditions in the Certificate of Analysis. Room temperature in continental US may vary elsewhere. Fasudil (HA-1077 AT877) is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively. Fasudil is also a potent Ca2+ channel antagonist and vasodilator. Fasudil (100 μM) inhibits cell spreading, the formation of stress fibers, and expression of α-SMA with concomitant suppression of cell growth in rat HSCs (hepatic stellate cells) and human HSC-derived TWNT-4 cells[4]. Fasudil (50-100 μM 24 hours) inhibits the LPA (lysophoaphatidic acid)-induced phosphorylation of ERK1/2, JNK, and p38 detected by western blotting in rat HSCs and human HSC-derived TWNT-4 cells[4]. Fasudil (25-100 μM 24 hours) suppresses transcription of collagen and TIMP, stimulates transcription of MMP-1 in human HSC-derived TWNT-4 cells[4]. Fasudil (10 mg/kg i.v. 1 h before operation) exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury[5]. Fasudil (50 mg/kg/d i.p.) inhibits acute and relapsing EAE (experimental autoimmune encephalomyelitis) induced by proteolipid protein PLP p139-151, reduces lymphocytes proliferation, results downregulation of interleukin (IL)-17 and a marked decrease of the IFN-γ/IL-4 ratio[6]. Fasudil (100 mg/kg/d p.o.) significantly reduces incidence and pathological examination score of EAE (experimental autoimmune encephalomyelitis) in SJL/J mice, decreases inflammation, demyelination, axonal loss and APP positivein spinal cord in mice[6]. p160ROCK 0.33 μM (Ki) ROCK2 0.158 μM (IC50) PKA 4.58 μM (IC50) PKC 12.3 μM (IC50) PKG 1.65 μM (IC50) \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief] [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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