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.

MedKoo Cat#: 407104 Name: Fasudil hydrochloride CAS#: 105628-07-7 (HCl); 103745-39-7 (Free base) Chemical Formula: C14H18ClN3O2S Exact Mass: Molecular Weight: 327.827 Elemental Analysis: C, 51.29; H, 5.53; Cl, 10.81; N, 12.82; O, 9.76; S, 9.78

Synonym: HA-1077; HA1077; HA 1077; HA-1077 HCl; Fasudil hydrochloride.

IUPAC/Chemical Name: 5-((1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

InChi Key: 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 Code: O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.[H]Cl

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

Additional Information

ROCK is an enzyme that plays an important role in mediating vasoconstriction and vascular remodeling in the pathogenesis of PH. ROCK induces vasoconstriction by phosphorylating the myosin-binding subunit of myosin light chain (MLC) phosphatase, thus decreasing MLC phosphatase activity and enhancing vascular smooth muscle contraction.

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.

6: Shibuya M, Asano T, Sasaki Y. Effect of Fasudil HCl, a protein kinase inhibitor, on cerebral vasospasm. Acta Neurochir Suppl. 2001;77:201-4. Review. PubMed PMID: 11563286.

7: Seto M, Takuwa Y, Sasaki Y. [The molecular mechanism of vasospasm and the attenuation by fasudil]. Nihon Yakurigaku Zasshi. 1999 Oct;114 Suppl 1:66P-70P. Review. Japanese. PubMed PMID: 10629857.

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