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Fasudil dihydrochloride

Cat. No.:YN252103

  • CAS No. :203911-27-7

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    • 产品名称: Fasudil dihydrochloride
      CAS No.: 203911-27-7
      Chemical Name: hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine, dihydrochloride
      Synonyms:HA-1077 dihydrochloride; AT-877 dihydrochloride
      分子量:364.3
      分子式:C14H17N3O2S • 2HCl
      SMILES:O=S(C1=CC=CC2=CN=CC=C21)(N3CCNCCC3)=O
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: Fasudil (HA-1077; AT877) dihydrochloride 是一种非特异性RhoA/ROCK抑制剂,并抑制蛋白激酶。Fasudil dihydrochloride 抑制ROCK1的Ki为 0.33 μM,抑制ROCK2,PKA,PKC,PKG的IC50分别为 0.158 μM 和 4.58 μM,12.30 μM,1.650 μM。Fasudil dihydrochloride 也是一种有效的 Ca2+通道拮抗剂和血管扩张剂。
      IC50和靶点: [{name:"PKA:4.58 μM (IC50)"},{name: "PKC:12.3 μM (IC50)"},{name: "p160ROCK:0.33 μM (Ki)"},{name: "ROCK2:0.158 μM (IC50)"},{name: "PKG:1.65 μM (IC50)"}]
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      In Vivo:
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    • Tawara, S., and Shimokawa, H.Progress of the study of Rho-kinase and future perspective of the inhibitorYakugaku Zasshi127(3),501-514(2007)

      Davies, S.P., Reddy, H., Caivano, M., et al.Specificity and mechanism of action of some commonly used protein kinase inhibitorsBiochem. J.351(1),95-105(2000)

      Oka, M., Homma, N., Taraseviciene-Stewart, L., et al.Rho kinase-mediated vasoconstriction is important in severe occlusive pulmonary arterial hypertension in ratsCirc. Res.100(6),923-929(2007)

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

      Kikuchi, Y., Yamada, M., Imakiire, T., et al.A Rho-kinase inhibitor, fasudil, prevents development of diabetes and nephropathy in insulin-resistant diabetic ratsJ. Endocrinol.192(3),595-603(2007)

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