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.
For research use only. We do not sell to patients.
- CAS No.: 2299200-91-0
- Formula: C23H24N4O5S
- Molecular Weight:468.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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All P2Y Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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P2Y12 Receptor |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
In Vivo
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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Molecular Weight 468.53
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Formula 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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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)
P2Y12 antagonist 2 Related Classifications
HY-111755 Related Classifications
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