1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride Property

Density 

1.289

RTECS 

HM4031166

Flash point:

260℃

storage temp. 

Store at -20°C

solubility 

H2O: >10mg/mL

form 

solid

color 

white to off-white

Water Solubility 

Soluble in water and dimethylsulfoxide.

Safety

Safety Statements 

24/25

WGK Germany 

3

HS Code 

29339900

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

1-(5-Isoquinolinylsulfonyl)homopiperazine dihydrochloride, Fasudil dihydrochloride Chemical Properties,Usage,Production

Description

Rho-associated kinase (ROCK), an effector of the small GTP-binding protein Rho, plays an important role in various cellular functions including vascular smooth muscle contraction, proliferation, and migration as well as inflammatory cell mobility. HA-1077 is a potent inhibitor of ROCK2 and additionally 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) with IC₅₀ values of 1.9, 4, 5, and 15 μM, respectively. By inhibiting the activity of ROCK, HA-1077 has been shown to reduce blood vessel constriction, decrease pulmonary arterial pressure, inhibit tumor angiogenesis, and improve insulin signaling in various rodent models. While originally marketed for the prevention of cerebral vasospasm in patients with subarachnoid hemorrhage, oral formulations of HA-1077 are used for the treatment of a wide range of cardiovascular diseases including pulmonary arterial hypertension and stable angina.

Chemical Properties

White fine crystalline powder

Uses

Fasudil dihydrochloride is used in the inhibition of contractile responses to potassium chloride, phenylephnne (PHE), prostaglandin and hepatic stellate cells spreading. It is also used in the formation of stress fibers and in medicine.

Uses

HA-1077 dihydrochloride has been used:

• to relax cantilevers
• in the functional assessment of isolated coronary arteries
• to investigate the effect of azaindole-1, fasudil on acute hypoxic pulmonary vasoconstriction (HPV)

Biochem/physiol Actions

Novel vasodilator agent which inhibits vascular smooth muscle contraction by acting as an intracellular Ca2+ antagonist.