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F-4660 Fasudil, Monohydrochloride Salt, >99%       Prices Reduced (November 2011)

[HA-1077, Monohydrochloride Salt] [1-(5-Isoquinolinesulfonyl)homopiperazine, Monohydrochloride Salt] [Eril] [AT-877] [HA1077] [HA 1077]

M.W. 327.83

C14H17N3O2S•HCl

[105628-07-7]

M.I. 12:  3980

M.I. 14:  3942

Storage:  Store at or below -20 ºC.  Solubility:  Very soluble in water, up to about 200 mg/mL ; soluble in DMSO up to about 95 mg/mL; not soluble in ethanol; addition of an aqueous solution of this monohydrochloride salt into a buffer solution may significantly alter its solubility.  Disposal:  A

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• Nomenclature.  Two names have been widely used for this compound, "HA-1077" and "Fasudil", and these names have been variously and inconsistently applied to the free base, the monohydrochloride salt and the dihydrochloride salt forms.  For many years LC Labs has sold the dihydrochloride salt under the name HA-1077, Dihydrochloride Salt, Cat. No. H-2330.  For historical reasons and for continuity, we have elected to continue using the HA-1077 name for our dihydrochloride salt product, even though we recently introduced the monohydrochloride salt form under the name Fasudil, Monohydrochloride Salt, Cat. No. F-4660, as described on this page.

• The monohydrochloride salt is the form used to prepare formulations of this drug for clinical use.  Note that the solubility properties of the mono- and di-HCl salts are different.

• Kinase inhibitor; has antivasospastic properties.
  -- Asano, T., et al.  "Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinases."  Br. J. Pharmacol. 98:  1091-1100 (1989).
  -- Sasaki, Y. and Sasaki, Y.  "Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator."  Biochem. Biophys. Res. Commun. 171:  1182-1187 (1990).
  -- Seto, M., et al.  "Effects of HA 1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle."  Eur. J. Pharmacol. 195:  267-272 (1991).
  -- Shibuya, O., et al.  The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:  53 (1988).
  -- Shirotani, M. et al.  "A new type of vasodilator, HA 1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture."  J. Pharmacol. Exp. Ther. 259:  738-744 (1991).
  -- Swärd, K. et al.  "Inhibition of Rho-associated kinase blocks agonist-induced Ca2+ sensitization of myosin phosphorylation and force in guinea-pig ileum."  J. Physiol. 522:  33-49 (2000).
  -- Davies, S.P. et al.  "Specificity and mechanism of action of some commonly used protein kinase inhibitors."  Biochem. J. 351:  95-105 (2000).

• Potencies for inhibition of various kinases by Fasudil:
  

  Enzyme	IC50	Ki	Reference
  Rho-associated Kinase II	1.9 µM		Davies, S.P. et al.
  Protein Kinase C-Related Kinase 2	4 µM		Davies, S.P. et al.
  Mitogen- and Stress-Activated Protein Kinase 1	5 µM		Davies, S.P. et al.
  Mitogen Activated Protein Kinase-Activated Protein Kinase 1b	5 µM		Davies, S.P. et al.
  Rho-associated Kinase	10.7 µM		Swärd, K. et al.
  Myosin Light Chain Kinase	95.2 µM		Swärd, K. et al.
  Protein Kinase C	425 µM		Swärd, K. et al.
  Cyclic AMP-Dependent Protein Kinase		1.6 µM	Asano, T. et al.
  Cyclic GMP-Dependent Protein Kinase		1.6 µM	Asano, T. et al.
  Myosin Light Chain Kinase		36 µM	Asano, T. et al.

• This monohydrochloride salt form is the active ingredient in drug formulations marketed in Japan to treat cerebral vasospasm following surgery for subarachnoid hemorrhage and associated cerebral ischemic symptoms.  Zhao, J. et al.  "Effect of Fasudil Hydrochloride, a Protein Kinase Inhibitor, on Cerebral Vasospasm and Delayed Cerebral Ischemic Symptoms After Aneurysmal Subarachnoid Hemorrhage."  Neurologia Medico-Chirurgica 46:  421-428 (2006).  Also, the monohydrochloride form has been or presently is in human clinical trials for treatment of acute cerebral thrombosis, subarachnoid hemorrhage, and angina pectoris.

• Regarding CAS Numbers:  the Chemical Abstracts Service (CAS) has assigned the number 103745-39-7 to the free base form of this compound (a form that LC Labs does not sell).  CAS has also assigned a different number, 105628-07-7, to the monohydrochloride salt form described on this page.  CAS apparently has not assigned a separate number to the dihydrochloride salt, so for our dihydrochloride salt product (see HA-1077, Dihydrochloride Salt, Cat. No. H-2330), we have used the number that CAS has assigned to the free base.

• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.