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HA-1077 (hydrochloride)

Cayman Chemical Item Number 10010559

Eril; Fasudil; AT-877 (CAS 203911-27-7)

HA-1077 (hydrochloride) (CAS 203911-27-7)

See more	Inhibitors (493) Angiogenesis (29) Atherosclerosis (323) Cancer (606) Cell Biology (281) Diabetes (134) Hypertension (90) Metabolism (139) Renal Disease (32) Vascular Disease (103)

Description

Rho-kinase, 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.¹HA-1077 is a potent inhibitor of Rho-associated Kinase II (ROCK-II) 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.² By inhibiting the activity of Rho-kinase, HA-1077 has been shown to reduce blood vessel constriction³, decrease pulmonary arterial pressure³, inhibit tumor angiogenesis⁴, and improve insulin signaling⁵ 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.

1 Tawara, S., and Shimokawa, H. Progress of the study of Rho-kinase and future perspective of the inhibitor. Yakugaku Zasshi 127(3) 501-514 (2007).

2 Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351 95-105 (2000).

3 Oka, M., Homma, N., Taraseviciene-Stewart, L., et al. Rho kinase-mediated vasoconstriction is important in severe occlusive pulmonary arterial hypertension in rats. Circ Res 100 923-929 (2007).

4 Yin, L., Morishige, K., Takahashi, T., et al. Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Mol Cancer Ther 6(5) 1517-1525 (2007).

5 Kikuchi, Y., Yamada, M., Imakiire, T., et al. A Rho-kinase inhibitor, fasudil, prevents development of diabetes and nephropathy in insulin-resistant diabetic rats. J Endocrinol 192 595-603 (2007).

Synonyms	Eril Fasudil AT-877
Formal Name	hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine, dihydrochloride
CAS Number	203911-27-7
Molecular Formula	C₁₄H₁₇N₃O₂S · 2HCl
Formula Weight	364.3
Formulation	A crystalline solid
Purity	≥98%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard O=S(C1=CC=CC2=CN=CC=C21)(N3CCNCCC3)=O

Background Reading

Oka, M., Homma, N., Taraseviciene-Stewart, L., et al. Rho kinase-mediated vasoconstriction is important in severe occlusive pulmonary arterial hypertension in rats. Circ Res 100 923-929 (2007).

Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J 351 95-105 (2000).

Tawara, S., and Shimokawa, H. Progress of the study of Rho-kinase and future perspective of the inhibitor. Yakugaku Zasshi 127(3) 501-514 (2007).

Kikuchi, Y., Yamada, M., Imakiire, T., et al. A Rho-kinase inhibitor, fasudil, prevents development of diabetes and nephropathy in insulin-resistant diabetic rats. J Endocrinol 192 595-603 (2007).

Yin, L., Morishige, K., Takahashi, T., et al. Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Mol Cancer Ther 6(5) 1517-1525 (2007).

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HA-1077 (hydrochloride) is available in the following screening library:

Kinase Screening Library (96-Well)

Size	Price	Quantity	Subtotal
5 mg	$46.00		$0.00
50 mg	$368.00		$0.00
100 mg	$644.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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