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Chemical Characteristic

Product Namebay 73-6691
CAS No.794568-92-6
Molecular Weight 356.73
FormulaC15H12ClF3N4O
Chemical Name1-(2-Chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
Smilesc1(nc2c(c(=O)[nH]1)cnn2c1c(cccc1)Cl)C[C@H](C(F)(F)F)C
Chemical Structure

Biological activities

BAY 73-6691 is a potent and selective inhibitor of phosphodiesterase 9(PDE9). BAY 73-6691 inhibits human recombinant PDE9 and murine PDE9 with IC50s of 55 and 100 nM, respectively.[1] BAY 73-6691 is widely used for treatment of Alzheimer?? disease. Meanwhile, BAY 73-6691 implicates in suppression of tumour growth both in vitro and in vivo.[1] In vitro, BAY 73-6691 significantly inhibits both MCF-7 and MDA-MB-468 cells proliferation in a time- and dose-dependent manner. Furthermore, BAY 73-6691 induces apoptosis in breast cancer cell lines through the cGMP pathway.[2] In vivo, BAY 73-6691 has been shown to improve learning and memory in rats.[3]

Protocols

In vivo, Bay 73-6691 is dissolved in solutol:ethanol:water (10:5:85).[3]

References

[1] Wunder F, et al. Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line. Mol Pharmacol. 2005, 68(6):1775-1781.
[2] Saravani R, et al. Inhibition of phosphodiestrase 9 induces cGMP accumulation and apoptosis in human breast cancer cell lines, MCF-7 and MDA-MB-468. Cell Prolif. 2012, 45(3):199-206.
[3] van der Staay FJ, The novel selective PDE9 inhibitor BAY 73-6691 improves learning and memory in rodents. Neuropharmacology. 2008, 55(5):908-918.

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