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PKC&ROCK

Fasudil hydrochloride (105628-07-7)

Fasudil Hcl(HA-1077; AT-877) 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, respectively.

Not Intended for Therapeutic Use. For research use only.

CAS: 105628-07-7 Category

Fasudil hydrochloride (105628-07-7) Description

Fasudil, also known as HA-1077, is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used 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. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February 2009 that fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients. It is approved for use in Japan and China.

Studies suggest that when acting as a ROCK inhibitor, Fasudil reduces neutrophil transendothelial migration by diminishing cytoskeletal rearrangement of endothelial cells. In addition, Fasudil significantly protects against MeHg-induced axonal degeneration and apoptotic cell death in cultured cortical neurons. Alternate studies show that Fasudil plays an important role in osteoblastic differentiation of stromal cells via increasing the mRNA expression of collagen-I, osteocalcin, and bone morphogenetic protein-2 (BMP-2).

Fasudil hydrochloride (105628-07-7) Specifications

Product Name Fasudil hydrochloride
Synonym HA-1077; HA1077; HA 1077; HA-1077 HCl; Fasudil hydrochloride.
Chemical Name 5-((1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 105628-07-7
Molecular Formula C14H17N3O2S•HCl
Molecular Weight 327.827
Monoisotopic Mass 327.8 g/mol
MDL number MFCD00943198
InChIKey LFVPBERIVUNMGV-UHFFFAOYSA-N
InChi Code InChI=1S/C14H17N3O2S.ClH/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;1H
SMILES O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.[H]Cl
Form Solid powder
Color White to off-white
Solubility  Soluble in water (200 mg/mL), and DMSO (95 mg/mL). Insoluble in ethanol.
Storage Temp.  -20°C
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application A potent Rho-kinase inhibitor and vasodilator

 


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RIDADR NONH for all modes of transport

References:

[1]. Shi J, Wei L. Rho kinases in cardiovascular physiology and pathophysiology: the effect of fasudil. J Cardiovasc Pharmacol. 2013 Oct;62(4):341-54. doi: 10.1097/FJC.0b013e3182a3718f. Review. PubMed PMID: 23921309; PubMed Central PMCID: PMC3884946.

[2]. Chen M, Liu A, Ouyang Y, Huang Y, Chao X, Pi R. 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. doi: 10.1517/13543784.2013.778242. Epub 2013 Mar 5. Review. PubMed PMID: 23461757.

[3]. Raja SG. Evaluation of clinical efficacy of fasudil for the treatment of pulmonary arterial hypertension. Recent Pat Cardiovasc Drug Discov. 2012 Aug;7(2):100-4. Review. PubMed PMID: 22670803.

[4]. Kitazono T. [Fasudil hydrochloride]. Nihon Rinsho. 2006 Oct 28;64 Suppl 7:617-21. Review. Japanese. PubMed PMID: 17461215.

[5]. Ishida T, Takanashi Y, Kiwada H. Safe and efficient drug delivery system with liposomes for intrathecal application of an antivasospastic drug, fasudil. Biol Pharm Bull. 2006 Mar;29(3):397-402. Review. PubMed PMID: 16508135.