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

• 価格
• 構造式
• 製品情報
• 製品詳細
• 文献

価格

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構造式

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製品情報

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 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. 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.

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製品詳細

name	HA-1077 (hydrochloride)
Formal Name	hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine, dihydrochloride
CAS Number	203911-27-7
Synonyms	Fasudil
Molecular Formula	C14H17N3O2S • 2HCl
Formula Weight	364.3
Purity	≥98%
Formulation	A crystalline solid
λmax	217 nm
SMILES	O=S(C1=CC=CC2=CN=CC=C21)(N3CCNCCC3)=O
InChI Code	InChI=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	NGOGFTYYXHNFQH-UHFFFAOYSA-N
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
Stability	≥ 2 years

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文献

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(1), 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. Circulation Research 100, 923-929 (2007).

4. Yin, L., Morishige, K.i., Takahashi, T., et al. Fasudil inhibits vascular endothelial growth factor-induced angiogenesis in vitro and in vivo. Molecular Cancer Therapeutics 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. Journal of Endocrinology 192, 595-603 (2007).

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