HA-1077 (dihydrochloride)

HA-1077 (dihydrochloride)

10 mg

Cat. No.: 61-F49

$99.00

HA-1077 is a potent inhibitor of Rho-associated kinase II (ROCK-II), and also inhibits Protein Kinase C-related kinase 2 (PRK2),  Mitogen- and Stress-Activated Protein Kinase (MSK1), and Mitogen Activated Protein Kinase-Activated Protein Kinase 1b (MAPKAP-K1b). HA-1077 is a novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist. Through the inhibition of Rho-kinase, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in rodent models.

 

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TECHNICAL INFORMATION

Other Names: hexahydro-​1-​(5-​isoquinolinylsulfonyl)-​1H-​1,​4-​diazepine,​ dihydrochloride, Eril, Fasudil

Chemical Formula:  C14H17N3O2S · 2HCl 

CAS Number: 203911-27-7

Molecular Weight: 364.3

Purity:  >98%

Appearance:  a crystalline solid 

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store  aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO up to 10mg/ml. Soluble in water up to 200 mg/ml. If precipitate is observed,  vortex for 5 minutes.

 

References

Yin et al. (2007) Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Mol Cancer Ther. 6(5):1517-25.

Shirotani et al. (1991) A new type of vasodilator | HA1077 | an isoquinoline derivative | inhibits proliferation of bovine vascular smooth muscle cells in culture. J Pharmacol Exp Ther. 259(2):738-44.

Nagumo et al. (2000) Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells. Am J Physiol Cell Physiol. 278(1):C57-85.

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