ALEXIS Biochemicals: HA-1100 . hydrochloride

ALX-270-451

Revised 20-Jun-08

HA-1100 . hydrochloride
SYNONYMS	Hydroxyfasudil 1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Rho-associated Protein Kinases [ROCK] / Related Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-451-M001		1 mg	40.00 USD
ALX-270-451-M005		5 mg	120.00 USD

Product Specification

FORMULA:	C₁₄H₁₇N₃O₃S . HCl
MW:	307.4 . 36.5
CAS NUMBER:	105628-72-6
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in water (20mM, warm).
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stock solutions are stable for up to one month when stored at -20°C. However it is recommended to prepare fresh solutions if possible.
HANDLING:	After reconstitution, prepare aliquots and store at -20°C. Protect from light. Packaged under inert gas.

Product Description

Cell permeable, hydroxylated metabolite of HA-1077 . 2HCl (Fasudil) (Prod. No. ALX-270-071) that displays anti-anginal properties. Acts as an ATP-competitive and reversible inhibitor of Rho kinase (ROCK) with ~100-fold greater selectivity over MLCK, MRCKβ and PKC. Inhibits coronary arteriosclerotic lesion formation. Increases osteocalcin expression and has beneficial effects on pulmonary hypertension.

Product Specific Literature References

Rho-kinase-mediated pathway induces enhanced myosin light chain phosphorylations in a swine model of coronary artery spasm: H. Shimokawa, et al.; Cardiovasc. Res. 43, 1029 (1999) Abstract
Hydroxyfasudil, an active metabolite of fasudil hydrochloride, relaxes the rabbit basilar artery by disinhibition of myosin light chain phosphatase: K. Nakamura, et al.; J. Cereb. Blood Flow Metab. 21, 876 (2001) Abstract
Pitavastatin enhanced BMP-2 and osteocalcin expression by inhibition of Rho-associated kinase in human osteoblasts: K. Ohnaka, et al.; BBRC 287, 337 (2001) Abstract
Antianginal effects of hydroxyfasudil, a Rho-kinase inhibitor, in a canine model of effort angina: T. Utsunomiya, et al.; Br. J. Pharmacol. 134, 1724 (2001) Abstract
Rho-kinase mediates hypoxia-induced downregulation of endothelial nitric oxide synthase: M. Takemoto, et al.; Circulation 106, 57 (2002) Abstract
Rho-kinase as a novel therapeutic target in treatment of cardiovascular diseases: H. Shimokawa; J. Cardiovasc. Pharmacol. 39, 319 (2002) Abstract
Essential role of rho kinase in the Ca2+ sensitization of prostaglandin F(2alpha)-induced contraction of rabbit aortae: K. Ito, et al.; J. Physiol. 546, 823 (2003) Abstract
Inhibition of Rho-kinase leads to rapid activation of phosphatidylinositol 3-kinase/protein kinase Akt and cardiovascular protection: S. Wolfrum, et al.; Arterioscler. Thromb. Vasc. Biol. 24, 1842 (2004) Abstract
Beneficial effect of hydroxyfasudil, a specific Rho-kinase inhibitor, on ischemia/reperfusion injury in canine coronary microcirculation in vivo: T. Yada, et al.; J. Am. Coll. Cardiol. 45, 599 (2005) Abstract
Inhibition of Rho kinase (ROCK) leads to increased cerebral blood flow and stroke protection: Y. Rikitake, et al.; Stroke 36, 2251 (2005) Abstract
The structure of dimeric ROCK I reveals the mechanism for ligand selectivity: M. Jacobs, et al.; J. Biol. Chem. 281, 260 (2006) Abstract
Sustained Elevation of Serum Cortisol Level Causes Sensitization of Coronary Vasoconstricting Responses in Pigs In Vivo. A Possible Link Between Stress and Coronary Vasospasm: T. Hizume, et al.; Circ. Res. 99, 767 (2006) Abstract; Full Text

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