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Art. -Nr.: HY-175675

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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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CAS. Nr.: 3104888-50-5
Formel: C₂₁H₁₁F₅N₄O₂
Molecular Weight:446.33

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

P2Y1 antagonist 4 Chemical Structure

CAS. Nr.: 3104888-50-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

P2Y1 Receptor

Alle P2Y Receptor Isoform-spezifische Produkte anzeigen :

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.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-∞	MRT_0-∞	CL	F
Rat^[1]	10 mg/kg	i.v.	3.67 h	0.14 h	39.19 μg/mL	28.49 μg·h/mL	1.85 h	5.85 mL/min/kg	/
Rat^[1]	10 mg/kg	p.o.	12.4 h	4.45 h	0.0546 μg/mL	0.78 μg·h/mL	/	/	2.7 %

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.

Chemical Information

CAS. Nr. 3104888-50-5
Molecular Weight 446.33
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang B, et al. Discovery of 1-Difluoromethyl-3-(3-cyanophenyl)-6-[4-(trifluoromethoxy)phenyl]imidazo[1,5-a]pyrazin-8-(7H)-one as a Potent P2Y1 Antagonist for the Treatment of Ischemic Stroke and Myocardial Infarction. J Med Chem. 2025 Aug 28;68(16):17990-18015. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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