Y-590

Y-590 is an orally active platelet cyclic adenosine monophosphate phosphodiesterase (cAMP-PDE) inhibitor with an IC₅₀ of 0.9 nM against rabbit cAMP-PDE. Y-590 inhibits platelet aggregation, disaggregates aggregated platelets, suppresses collagen-induced platelet release, reduces platelet retention and inhibits cAMP degradation in platelets. Y-590 enhances PGI₂-mediated elevation of intracellular cAMP in platelets and exerts a synergistic effect with PGI₂ on ADP-induced platelet aggregation. Y-590 can be used in studies related to thrombotic diseases and thrombosis^[1][2]. In Vitro:Y-590 (2 min) inhibits ADP (HY-W010918)-, Collagen (HY-NP003)-, and Arachidonic acid (AA) (HY-109590)-induced platelet aggregation in platelet-rich plasma from rats, rabbits, and guinea pigs in a dose-dependent manner, with IC₅₀ values ranging from 9 ng/mL to 110 ng/mL depending on the species and aggregation inducer^[1].
Y-590 (30-1000 ng/mL; added 1 min after AA-induced aggregation) induces dose-dependent disaggregation of AA-preaggregated guinea pig platelets, with activity detectable at a concentration of 30 ng/mL^[1].
Y-590 (administered 2 minutes before collagen treatment; co-incubated with collagen for 5 minutes) dose-dependently inhibits collagen-induced serotonin release in rabbit platelets, with an IC₅₀ of 12 ng/mL^[1].
Y-590 (administered 2 min prior to AA treatment; co-incubated with AA for 5 min at concentrations of 0.1-1 μg/mL) inhibits AA-induced platelet aggregation^[1].
Y-590 (0.1-1 μM; 1.5-2 min) enhances PGI₂-induced elevation of intracellular cAMP in washed rabbit platelets^[2].
Y-590 (5 min) potently and selectively inhibits rabbit platelet cAMP-PDE with an IC₅₀ of 0.9 nM, whereas it exhibits much weaker inhibitory activity against rabbit platelet cGMP-PDE with an IC₅₀ of 95 μM, resulting in a high G/A selectivity ratio of up to 1055^[2].
Y-590 (preincubated for 2 min prior to ADP addition) potently inhibits ADP-induced platelet aggregation in rabbit platelet-rich plasma (PRP), with an IC₅₀ of 0.36 nM, and its efficacy is comparable to its cAMP-PDE inhibitory activity^[2].
Y-590 (0.3-1 ng/mL; administered 2 min prior to ADP addition) acts synergistically with PGI₂ (3 pg/mL; added 1.5 minutes after Y-590) to inhibit ADP-induced aggregation of rabbit platelet-rich plasma^[1]. In Vivo:Y-590 (0.01-0.3 mg/kg; p.o.; single administration) dose-dependently inhibits ADP-induced platelet aggregation in male Sprague-Dawley rats at 2 hours post-administration^[1].
Y-590 (0.03 mg/kg; p.o.; single administration) inhibits ADP-induced platelet aggregation in male albino rabbits with a duration of action of at least 12 h^[1].
Y-590 (0.03-1.0 mg/kg; p.o.; single administration) dose-dependently inhibits platelet retention in male Hartley guinea pigs at 2 h post-administration, with an inhibition rate of 93% at the dose of 1.0 mg/kg^[1].