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P2Y1 antagonist 4

Catalog No. T212954 Copy Product Info
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P2Y1 antagonist 4 is a selective blocker of the P2Y1 receptor with excellent penetration across the blood-brain barrier. It inhibits ADP-induced increases in cytosolic Ca2+ mediated by the P2Y1 receptor in washed rabbit platelets (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM). P2Y1 antagonist 4 significantly elevates nuclear Nrf2 protein levels in H2O2-treated HT22 cells. It reduces infarct size in a mouse acute myocardial infarction model and is applicable in research on ischemic stroke and myocardial infarction.

P2Y1 antagonist 4

Copy Product Info
🥰Excellent
Catalog No. T212954

P2Y1 antagonist 4 is a selective blocker of the P2Y1 receptor with excellent penetration across the blood-brain barrier. It inhibits ADP-induced increases in cytosolic Ca2+ mediated by the P2Y1 receptor in washed rabbit platelets (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM). P2Y1 antagonist 4 significantly elevates nuclear Nrf2 protein levels in H2O2-treated HT22 cells. It reduces infarct size in a mouse acute myocardial infarction model and is applicable in research on ischemic stroke and myocardial infarction.

P2Y1 antagonist 4
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Description
P2Y1 antagonist 4 is a selective blocker of the P2Y1 receptor with excellent penetration across the blood-brain barrier. It inhibits ADP-induced increases in cytosolic Ca2+ mediated by the P2Y1 receptor in washed rabbit platelets (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM). P2Y1 antagonist 4 significantly elevates nuclear Nrf2 protein levels in H2O2-treated HT22 cells. It reduces infarct size in a mouse acute myocardial infarction model and is applicable in research on ischemic stroke and myocardial infarction.
In vitro
P2Y1 antagonist 4 (Compound 12g) inhibits the P2Y1 receptor-mediated increase in cytoplasmic Ca 2+ induced by ADP in washed rabbit platelets, with an IC50 of 1.95 μM, and also prevents platelet aggregation with an IC50 of 3.24 μM. At 10 μM for 24 hours, P2Y1 antagonist 4 significantly enhances cell viability in HT22 hippocampal neurons under H2O2-induced oxidative stress. Additionally, at 10 μM for 16 hours, it significantly upregulates the levels of nuclear Nrf2 protein in H2O2-treated HT22 cells.
In vivo
Compound 12g (P2Y1 antagonist 4) administered intravenously at 5-20 mg/kg immediately after LAD ligation, significantly reduces myocardial infarct size in male C57BL/6 mice in a dose-dependent manner and lowers serum CK-MB/LDH levels, evaluated over 24 hours.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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