P2Y12 antagonist 2
P2Y12 antagonist 2 is a potent P2Y12 receptor antagonist. P2Y12 antagonist 2 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. P2Y12 antagonist 2 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. P2Y12 antagonist 2 can be used to research thromboembolic disorders.
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- CAS No.: 2299200-91-0
- Formule: C23H24N4O5S
- Masse moléculaire:468.53
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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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Activité biologique
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P2Y12 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Platelet | IC50 |
2.94 μM
Compound: 58l
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Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation by aggregometry
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of ADP-induced platelet aggregation by aggregometry
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[PMID: 30843696] |
P2Y12 antagonist 2 (compound 58l) moderately inhibits CYP3A4 with an IC50 of about 1.5 μM, but exhibits weak inhibition in the other main subtypes (IC50>25 μM)[1].
P2Y12 antagonist 2 does not inhibit hERG even at 40 μM, indicating that it has no QT interval prolongation-related cardiac toxicity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
P2Y12 antagonist 2 (2.5-40 mg/kg; p.o.; single dosage) prolongs the bleeding time in tail-bleeding model rats[1].
P2Y12 antagonist 2 exhibits great stability in both rat and human liver microsomes with the low clearance values and long half-life [human: T1/2=208.3 min, Clint=10.1 mL/(min g protein); rats: T1/2=89.1 min, Clint=10.6 mL/(min g protein)][1].
P2Y12 antagonist 2 (5 mg/kg; p.o.; single dosage) exhibits excellent pharmacokinetic properties with relatively low clearance, high plasma exposure and good oral bioavailability in rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar rats (250-300 g, n = 10; FeCl3 thrombosis model)[1]
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Dosage:2.5, 5, 10, 20, 40 and 80 mg/kg
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Administration:p.o.; single dosage
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Result:Decreased thrombus weight in a dose-dependent manner with an ED50 of 27 mg/kg compared to that of 7 mg/kg for Clopidogrel (HY-15283).
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Animal Model:Male rats (250-300 g, n = 10; tail-bleeding model)[1]
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Dosage:2.5, 5, 10, 20 and 40 mg/kg
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Administration:p.o.; single dosage
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Result:Prolonged the bleeding time in a dose-dependent manner.
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Animal Model:Male Sprague-Dawley rats (200-220g)[1]
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Dosage:5 mg/kg
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Administration:p.o.; single dosage
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Result:Pharmacokinetic Parameters of Oral antiplatelet agent 1 (compound 58l) in male Sprague-Dawley rats[1].
Cmax (ng/mL) T1/2 (h) Tmax (h) AUC0-∞ (ng·h/mL) MRT (h) p.o. 5 mg/kg 1661 ± 642 2.91 ± 1.09 0.25 4120 ± 2127 3.64 ± 0.18
Chemical Information
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CAS No. 2299200-91-0
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Masse moléculaire 468.53
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Formule C23H24N4O5S
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SMILES
O=C(OC1)C2=C1N=C(N3CCC(C(NS(CC4=CC=C(C)C=C4)(=O)=O)=O)(C)CC3)C(C#N)=C2
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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)
P2Y12 antagonist 2 Related Classifications
HY-111755 Related Classifications
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