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HA1077 (Fasudil, 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine

Cat no: H1000-01

HA1077 (Fasudil, 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine

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.\n\nSolubility:\nVery soluble in water, up to 200mg/ml or more; soluble in DMSO up to about 10mg/ml; not soluble in ethanol; addition of an aqueous solution of this dihydrochloride salt into a buffer solution may significantly alter its solubility.\n\nStorage and Stability:\nMay be stored at RT for short-term only. Long-term storage is recommended at -20 degrees C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.

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SPECIFICATIONS

Catalog Number

H1000-01

Size

250mg

Form

Supplied as a white to off-white powder.

Purity

~99%

References

1. 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). 2. 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). 3. 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). 4. 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). 5. Shibuya, O., et al. The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs. Acta Neurochir. 90:53 (1988). 6. 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). 7. Sw

Alternative Names

HA-1077, Dihydrochloride Salt

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