AY 31390
AY 31390 is a potent PDE III inhibitor. AY 31390 increases intracellular cAMP levels by selectively inhibiting the low-Km cAMP-specific PDE III, thereby stabilizing platelets and exerting antithrombotic effects independently of plasma adenosine concentrations. AY 31390 can be used in the study of thrombosis, angina pectoris, cerebral ischemia, and peripheral vascular diseases.
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- CAS No.: 135124-72-0
- Formule: C11H11Br3N4O
- Masse moléculaire:454.94
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
PDE Ⅲ |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
0.18 μM
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Inhibition of arachidonic acid-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
Inhibition of arachidonic acid-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
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1896959 |
| Platelet | IC50 |
0.21 μM
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Inhibition of U46619-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
Inhibition of U46619-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
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1896959 |
| Platelet | IC50 |
0.54 μM
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Inhibition of collagen-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
Inhibition of collagen-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
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1896959 |
| Platelet | IC50 |
0.43 μM
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Inhibition of second-phase epinephrine-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
Inhibition of second-phase epinephrine-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
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1896959 |
| Platelet | IC50 |
0.20 μM
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Inhibition of second-phase ADP-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
Inhibition of second-phase ADP-induced aggregation in human platelets assessed via light transmission measurement following 3-minute pre-incubation with the reagent and 4-minute aggregation measurement.
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1896959 |
In Vitro
AY 31390 (3 min pre-incubation; 4 min aggregation assay) exerts a potent inhibitory effect on platelet aggregation induced by multiple agonists in human platelet-rich plasma, with IC50 values ranging from 0.18 μM to 0.54 μM depending on the agonist[1].
AY 31390 (1 μM; 30 min) reversibly inhibits human platelet aggregation induced by Collagen (HY-NP003) and Arachidonic acid (HY-109590), and its inhibitory activity disappears after washing and resuspension[1].
AY 31390 (0.25-1 μM; 5 min) exerts an anti-platelet aggregation effect in human platelet-rich plasma (PRP) pretreated with ADA (HY-D0855A), and its inhibitory effect on the Arachidonic acid system is not affected by ADA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:New Zealand rabbits (male, 2.0-2.5 kg)[1]
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Dosage:0.1 mg/kg; 0.25 mg/kg; 0.50 mg/kg
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Administration:i.v.; single bolus; 15 min
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Result:Reduced white thrombus formation by 28.4%.
Reduced white thrombus formation by 47.1%.
Reduced white thrombus formation by 59.7%.
Chemical Information
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CAS No. 135124-72-0
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Masse moléculaire 454.94
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Formule C11H11Br3N4O
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SMILES
O=C1N=C(C)NC(NCC2=CC(Br)=CN=C2)=C1Br.Br
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AY 31390 Related Classifications
HY-165437 Related Classifications
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