P2Y1 antagonist 4
P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction.
For research use only. We do not sell to patients.
- CAS No.: 3104888-50-5
- Formula: C21H11F5N4O2
- Molecular Weight:446.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All P2Y Receptor Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
P2Y1 Receptor |
In Vitro
P2Y1 antagonist 4 (Compound 12g) inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets[1].
P2Y1 antagonist 4 (10 μM, 24 h) significantly increases cell viability in H2O2-induced oxidative stress-injured HT22 hippocampal neurons[1].
P2Y1 antagonist 4 (10 μM, 16 h) significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The chest was opened at the fourth costal space of the left chest wall along the left edge of the sternum to expose the heart, and a 7-0 silk thread was threaded through a live knot 2 mm from the left anterior descending coronary artery (LAD) branch for permanent ligation in Male C57BL/6 mice (20-25 g, 5-6 weeks old)[1]
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Dosage:5, 10, 20 mg/kg
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Administration:i.v., single dose immediately post-LAD ligation, 24 h evaluation
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Result:Reduced myocardial infarct size dose-dependently.
Alleviated myocardial cytolysis and reduces fibrosis.
Chemical Information
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CAS No. 3104888-50-5
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Molecular Weight 446.33
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Formula C21H11F5N4O2
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SMILES
O=C1C2=C(C(F)F)N=C(C3=CC=CC(C#N)=C3)N2C=C(C4=CC=C(OC(F)(F)F)C=C4)N1
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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.
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Research Protocol for Cardiovascular Diseases
Cardiovascular disease can be modeled as maladaptive cardiac remodeling, where ischemic injury or pressure overload activates inflammatory signaling, fibroblast activation, extracellular-matrix deposition, cardiomyocyte hypertrophy, vascular remodeling, and progressive ventricular dysfunction. The TGF-β/SMAD axis is a central profibrotic pathway after myocardial injury and pressure overload, while innate immune and cytokine pathways regulate leukocyte recruitment, scar formation, and adverse remodeling. Key unresolved questions include which inflammatory signals are reparative versus harmful, when fibrosis is protective versus maladaptive, and whether pathway inhibition improves function without weakening necessary infarct healing or compensatory remodeling.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)