794568-92-6

Usage

Uses

Used in Cardiovascular Research:
BAY 73-6691 is used as a PDE9 inhibitor for ischemic heart samples, helping researchers study the effects of PDE9 inhibition on heart function and blood flow in conditions such as ischemia.
Used in Structural Studies:
BAY 73-6691 is used as a PDE9 inhibitor in structural studies, allowing researchers to investigate the molecular interactions between PDE9 and other molecules, which can provide insights into the development of new therapeutic agents.
Used in Neuroblastoma Research:
BAY 73-6691 may be used as a PDE9 inhibitor in neuroblastoma SH-SY5Y cells, a type of human neuroblastoma cell line. This application can help researchers explore the potential therapeutic effects of PDE9 inhibition in neuroblastoma, a type of cancer that arises from nerve cells.

Biochem/physiol Actions

BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. BAY 73-6691 selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.

InChI:InChI=1/C15H12ClF3N4O/c1-8(15(17,18)19)6-12-21-13-9(14(24)22-12)7-20-23(13)11-5-3-2-4-10(11)16/h2-5,7-8,20H,6H2,1H3/t8-/m1/s1