HA-1077 (hydrochloride)

Cayman Chemical Item Number 10010559

(CAS 203911-27-7)

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

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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).

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%
λmax 217 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=S(C1=CC=CC2=CN=CC=C21)​(N3CCNCCC3)​=O
InCHI Code
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​1S/C14H17N3O2S/c18-20(19,17-9-2-6-15-8-10-17)​14-4-1-3-12-11-16-7-5-13(12)​14/h1,3-5,7,11,15H,2,6,8-10H2
InCHI Key
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NGOGFTYYXHNFQH-UHFFFAOYSA-N

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

Size Price Quantity Subtotal
5 mg $46.00 $0.00
10 mg $87.00 $0.00
50 mg $368.00 $0.00
100 mg $644.00 $0.00
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Pricing updated 2014-04-23. Prices are subject to change without notice.

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