베이41-2272

개요Soluble guanylate cyclase (sGC), a receptor for nitric oxide (NO), is a heterodimer consisting of alpha and beta subunits, with the beta subunit featuring a heme-nitric oxide (H-NOX) binding domain. The binding of NO to H-NOX induces sGC to generate the second messenger cGMP. BAY 41-2272 is a pyrazolopyridine compound that acts as an activator of sGC, stimulating activity to a level that would be expected to cause biologically important increases in cGMP at concentrations as low as 10-100 nM. Through this effect, it inhibits platelet aggregation (IC50 = 36 nM), induces relaxation of phenylephrine-preconstricted rabbit aorta rings (IC50 = 304 nM), and reduces proliferation in smooth muscle. BAY 41-2272 is effective in vivo, as it decreases mean arterial blood pressure in hypertensive rats. Unlike another sGC activator, YC-1 , BAY 41-2772 does not inhibit phosphodiesterases.

용도BAY 41-2272 is a soluble guanylate cyclase agonist that activates human mononuclear phagocytes. Inhibits vascular smooth muscle growth through the cAMP-dependent protein kinase and cGMP-dependent protein kinase pathways.

일반 설명A cell-permeable pyrazolopyridinylpyrimidine compound that acts as a selective and potent stimulator of soluble guanylate cyclase (effective dose ~ 0.1 nM to 100 μM using recombinant soluble guanylate cyclase). The mode of activation is NO-independent and appears to be mediated through direct binding to the α1 and α2 subunits. Shown to be effective in treating numerous cardiovascular conditions in animal models. Inhibits phenylephrine-induced constriction of rabbit aortic rings (IC50 = 304 nM) and blocks collagen-induced aggregation of human platelets (IC50 = 36 nM). Does not inhibit phosphodiesterases.