Drug intelligence / Profile preview

PF-04957325

Development stage
Unknown
Modality
Small Molecules
Administration
Subcutaneous
01

Overview

PF-04957325 is a highly potent, selective, small-molecule inhibitor of phosphodiesterase 8 (PDE8), targeting both PDE8A and PDE8B isoforms with sub-nanomolar IC50 values. Developed by Pfizer, the compound acts by preventing the hydrolysis of cyclic adenosine monophosphate (cAMP), thereby enhancing intracellular cAMP signaling. In preclinical research, PF-04957325 has been shown to stimulate steroidogenesis in adrenal and Leydig cells, suppress T-cell adhesion to endothelial cells (with implications for autoimmune encephalomyelitis and multiple sclerosis models), inhibit breast cancer cell migration, and improve cognitive function in Alzheimer's disease models by reducing microglial neuroinflammation. It is primarily utilized as a chemical probe and research tool.

Other names
3-[[(2R)-4-(1,3-thiazol-2-ylmethyl)morpholin-2-yl]methyl]-5-(trifluoromethyl)triazolo[4,5-d]pyrimidin-7-amine3-[[(2R)-4-(2-Thiazolylmethyl)-2-morpholinyl]methyl]-5-(trifluoromethyl)-3H-1,2,3-triazolo[4,5-d]pyrimidin-7-amine3-[[(2R)-4-(thiazol-2-ylmethyl)morpholin-2-yl]methyl]-5-(trifluoromethyl)triazolo[4,5-d]pyrimidin-7-amine
02

Targets

PDE8A (Phosphodiesterase 8A)

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