SB-772077B (dihydrochloride)

SB-772077B dihydrochloride is an orally active aminofuran-based Rho kinase ((ROCK)) inhibitor with IC₅₀ values of 5.6 nM and 6 nM for ROCK1 and ROCK2, respectively. SB-772077B dihydrochloride reduces inflammatory cytokines (TNF-α and IL-6). SB-772077B dihydrochloride relaxes aortic rings and lowers blood pressure. SB-772077B dihydrochloride can be used in the research of inflammatory diseases^[1][2]. IC50 & Target:IC50: 5.6 nM (ROCK1), 6 nM (ROCK2)^[1] In Vitro:SB-772077-B dihydrochloride exhibits an IC₅₀ value of 5.6 nM towards recombinant human ROCK1 and 6 nM towards human ROCK2^[1].
SB-772077-B (3 μM; 30 min before Angiotensin II stimulation) dihydrochloride completely abolishes the Angiotensin II (HY-13948)-induced actin stress fiber formation in human primary aortic smooth muscle cells^[1].
SB-772077-B (0.1-10 μM; 30 min before LPS) dihydrochloride dose-dependently reduces the production of LPS-induced inflammatory cytokines, including TNF-α and IL-6, in primary human macrophages^[1].
SB-772077-B dihydrochloride induces profound dose-dependent relaxation of Phenylephrine (HY-B0769)-precontracted rat aortic rings with an IC₅₀ of 39 nM^[1].
In Vivo:SB-772077-B (0.3-3 mg/kg; p.o.) dihydrochloride produces a profound reduction of blood pressure in spontaneously hypertensive rats and Deoxycorticosterone acetate (HY-B1472)- induced hypertensive rats^[1].