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HA1077 (Fasudil, 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine•2HCl, 1-(5-Isoquinolinesulfonyl) homopiperazine•2HCl)
HA1077 (Fasudil, 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine•2HCl,
1-(5-Isoquinolinesulfonyl) homopiperazine•2HCl)
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| A potent calcium antagonist vasodilator which is considered to act by employing different mechanisms from the usual calcium channel blockers since it inhibits (1) calcium ionophore A23187 induced contraction in arterial strips and (2) phenylephrine induced contraction in calcium free media suggesting that its site of action is in the intracellular space. Also reported to potently inhibit Rho-associated Kinase (ROCK). | | | Catalog # | H1000 | | HA1077 is an inhibitor of ROK/ROCK II (IC50 1.9uM), PRK2 (IC50 4uM), MSK1 (IC50 5uM), Rsk2 (IC50 15uM), PKA, p70 S6 Kinase, CaM Kinase (Ki 1.8nM) and MLCK (Ki 20nM). HA1077 is a calcium antagonist and has antivasospastic properties. Inhibits ROKa/ROCK II, PRK2, MSK1, Rsk2, PKA, p70 S6 Kinase, CaM Kinase and MLCK. | | Solubility | Methanol, Water | | Melting Point | >225º | | Method for Determining Identity | Proton NMR Spectroscopic Analysis; | | Conforms to structure | | TLC Conditions | SiO2; Dichloromethane: Methanol: Acetic Acid; 8:2:1; Visualized with UV and ninhydrin; Rf=0.3 | | Chloride content: 19.3% | | Storage and Stability | May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap. | | CAS Number | 103745-39-7 | | Molecular Formula | C14H19Cl2N3O2S•2HCl | | Molecular Weight | 402.75 | | Important Note | This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological. Toxicity and Hazards: All products should be handled by qualified personnel only, trained in laboratory procedures. | | Alternate names | 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine?2HCl; 1-(5-Isoquinolinesulfonyl) homopiperazine?2HCl) |
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