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.
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- CAS. Nr.: 70386-06-0
- Formel: C15H17N3O2
- Molecular Weight:271.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male)[1]
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Dosage:0.01 mg/kg; 0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited ex vivo ADP-induced platelet aggregation, with increasing inhibition observed across the tested dose range.
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Animal Model:albino (male)[1]
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Dosage:0.03 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited ex vivo ADP-induced platelet aggregation for at least 12 hours post-dose.
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Animal Model:Hartley (male)[1]
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Dosage:0.03 mg/kg; 0.1 mg/kg; 0.3 mg/kg; 1.0 mg/kg
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Administration:p.o.; single dose
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Result:Dose-dependently inhibited ex vivo platelet retention, producing 29% inhibition at 0.03 mg/kg.
Produced 37% inhibition at 0.1 mg/kg.
Produced 67% inhibition at 0.3 mg/kg.
Produced 93% inhibition at 1.0 mg/kg.
Chemical Information
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CAS. Nr. 70386-06-0
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Molecular Weight 271.31
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Formel C15H17N3O2
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SMILES
O=C1NN=C(C(C1)C)C2=CC(CCC(N3C)=O)=C3C=C2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Y-590 Related Classifications
HY-123366 Related Classifications
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