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BAY 73-6691

Cat. No. M7635

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BAY 73-6691 Structure
Synonym:

(R)-BAY 73-6691

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Quality Control & Documentation
Biological Activity

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. This compound 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.†

Chemical Information
Molecular Weight 356.73
Formula C15H12ClF3N4O
CAS Number 794568-92-6
Solubility (25°C) DMSO: ≥20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] Tsuyoshi Tajima, et al. Phosphodiesterase 9 (PDE9) regulates bovine tracheal smooth muscle relaxation

[2] Jian Li, et al. Protective effects of BAY 73-6691, a selective inhibitor of phosphodiesterase 9, on amyloid-β peptides-induced oxidative stress in in-vivo and in-vitro models of Alzheimer's disease

[3] Maritza Cavalcante Barbosa, et al. The Effect of a Selective Inhibitor of Phosphodiesterase-9 on Oxidative Stress, Inflammation and Cytotoxicity in Neutrophils from Patients with Sickle Cell Anaemia

[4] F H da Silva, et al. Phosphodiesterase-9 (PDE9) inhibition with BAY 73-6691 increases corpus cavernosum relaxations mediated by nitric oxide-cyclic GMP pathway in mice

[5] F Josef van der Staay, et al. The novel selective PDE9 inhibitor BAY 73-6691 improves learning and memory in rodents

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  Catalog
Abmole Inhibitor Catalog




Keywords: BAY 73-6691, (R)-BAY 73-6691 supplier, PDE, inhibitors, activators

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