HA1077 , Highly Purified (1-(5-Isoquinolinesulfonyl) homopiperazine.2HCl))

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). 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. , Synonyms:, Fasudil Dihydrochloride, 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine2HCl, 1-(5-Isoquinolinesulfonyl) homopiperazine2HCl), CAS No: 103745-39-7, Free Base: 103745-39-7, Molecular Formula: C14H17N3O2S2HCl, Molecular Weight: 364.29, Appearance: Supplied as a white to off-white powder. Purity: ~98%, Melting Point: >238ºC (dec), Solubility: Methanol (Slightly), Water (Slightly), Proton NMR (D2O) and Mass Spectrometric Analysis: Conforms to structure, TLC Conditions: C18, Methanol: Water: Acetic Acid, 8:2:0.05, Visualized with UV and ninhydrin, Rf=0.35, Chloride Content (Ion Chromatography): ~19%, 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.