A ROCK inhibitor
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Active Metabolite(s)
40814Hydroxyfasudil
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HA-1077 (hydrochloride)

Item No. 10010559

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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 (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 3 mg/mlPBS (pH 7.2): 5 mg/ml
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $49

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    50 mg

    $107

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    100 mg

    $167

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    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.1 HA-1077 is a potent inhibitor of ROCK2 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 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.3,4,5 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    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. Circ. Res. 100(6), 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. 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(3), 595-603 (2007).