2. GPCR/G Protein NF-κB
  3. P2Y Receptor Keap1-Nrf2
  4. 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.

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P2Y1 antagonist 4

P2Y1 antagonist 4 Chemical Structure

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P2Y1 antagonist 4 Related Antibodies

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Description

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[1].

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.

P2Y1 antagonist 4 Related Antibodies
In Vivo

P2Y1 antagonist 4 (Compound 12g) (5-20 mg/kg, i.v., single dose immediately post-LAD ligation, 24 h evaluation) reduces myocardial infarct size dose-dependently and lowers serum CK-MB/LDH in male C57BL/6 mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 5, 10, 20 mg/kg
Administration: i.v., single dose immediately post-LAD ligation, 24 h evaluation
Result: Reduced myocardial infarct size dose-dependently.
Alleviated myocardial cytolysis and reduces fibrosis.
Molecular Weight

446.33

Formula

C21H11F5N4O2
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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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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P2Y1 antagonist 4 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

P2Y1 antagonist 4P2Y ReceptorKeap1-Nrf2P2Y1 receptorischemic strokemyocardial infarctionNrf2Inhibitorinhibitorinhibit

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