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HA-1077

Rho kinase (ROCK) inhibitor
 
BML-EI233-0010 10 mg 125.00 USD
 
BML-EI233-0050 50 mg 520.00 USD
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Replaces Prod. #: ALX-270-071

Inhibits Rho kinase (ROCK; Ki=0.33μM). Selective protein kinase A and G inhibitor (both Ki’s = 1.6μM). Inhibits agonist-induced activation of NADPH oxidase in human neutrophils (IC50=15μM). Inhibitor of myosin light chain kinase and Ca2+/calmodulin-dependent protein kinase II. Inhibits translocation of PKCβI, PKCβII and PKCζ. Cell permeable Ca2+ antagonist with antivasospastic properties.

Product Specification

Alternative Name:1-(5-Isoquinolinesulfonyl)homopiperazine . 2HCl, Fasudil
 
Formula:C14H17N3O2S . 2HCl
 
MW:364.3
 
CAS:103745-39-7
 
MI:14: 3942
 
Purity:≥98% (TLC)
 
Identity:Determined by 1H-NMR and MS.
 
Appearance:White to off-white solid.
 
MeltingPoint:238-242°C
 
Solubility:Soluble in water (>20mg/ml), methanol or DMSO.
 
Shipping:Ambient
 
Long Term Storage:-20°C
 
Use/Stability:Stable for at least 1 year after receipt when stored, as supplied, at 0-4°C. Stock solutions are stable for up to 3 months at -20°C.
 
270-071
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270-071

Product Literature References

Effects of K-115 (Ripasudil), a novel ROCK inhibitor, on trabecular meshwork and Schlemm's canal endothelial cells: Y. Kaneko, et al.; Sci. Rep. 6, 19640 (2016), Application(s): Cell culture, Abstract; Full Text
Effects of HA-1077 and Y-27632, Two Rho-Kinase Inhibitors, in the Human Umbilical Artery: M. Ark, et al.; Cell Biochem. Biophys. 41, 331 (2004), Abstract;
Investigation of the inhibitory effects of HA-1077 and Y-32885 on the translocation of PKCbetaI, PKCbetaII and PKCzeta in human neutrophils: X. Siomboing, et al.; Mediators Inflamm. 10, 315 (2001), Abstract;
Rho kinase inhibitor HA-1077 prevents Rho-mediated myosin phosphatase inhibition in smooth muscle cells: H. Nagumo, et al.; Am. J. Physiol. Cell. Physiol. 278, C57 (2000), Abstract;
Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: U. M. Ishizaki, et al.; Nature 389, 990 (1997), Abstract;
Effects of isoquinoline derivatives, HA1077 and H-7, on cytosolic Ca2+ level and contraction in vascular smooth muscle: S. Takizawa, et al.; Eur. J. Pharmacol. 250, 431 (1993), Abstract;
Inhibition by the protein kinase inhibitor HA1077 of the activation of NADPH oxidase in human neutrophils.: M. Arai, et al.; Biochem. Pharmacol. 46, 1487 (1993), Abstract;
A new type of vasodilator, HA1077, an isoquinoline derivative, inhibits proliferation of bovine vascular smooth muscle cells in culture: M. Shirotani, et al.; J. Pharmacol. Exp. Ther. 259, 738 (1991), Abstract;
Effects of HA1077, a protein kinase inhibitor, on myosin phosphorylation and tension in smooth muscle: M. Seto, et al.; Eur. J. Pharmacol. 195, 267 (1991), Abstract;
Inhibition of myosin light chain phosphorylation in cultured smooth muscle cells by HA1077, a new type of vasodilator: Y. Sasaki & Y. Sasaki; BBRC 171, 1182 (1990), Abstract;
Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase: T. Asano, et al.; Br. J. Pharmacol. 98, 1091 (1989), Abstract;
The effects of an intracellular calcium antagonist HA 1077 on delayed cerebral vasospasm in dogs: O. Shibuya, et al.; Acta Neurochir. 90, 53 (1988), Abstract;
Mechanism of action of a novel antivasospasm drug, HA1077: T. Asano, et al.; J. Pharmacol. Exp. Ther. 241, 1033 (1987), Abstract;

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