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.
For research use only. We do not sell to patients.
- CAS No.: 70386-06-0
- Formula: C15H17N3O2
- Molecular Weight:271.31
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[2]|
cAMP-PDE 0.9 μM (IC50) |
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. Further protocols information, click here.
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 No. 70386-06-0
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Molecular Weight 271.31
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Formula C15H17N3O2
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SMILES
O=C1NN=C(C(C1)C)C2=CC(CCC(N3C)=O)=C3C=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)