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Art. -Nr.: HY-162408

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PAR4 antagonist 3

PAR4 antagonist 3 (Compound 36) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC₅₀ of 26.1 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T_1/2 of 97.6 min.

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CAS. Nr.: 3057206-40-0
Formel: C₂₂H₁₆FN₃O₅S
Molecular Weight:453.44

Speicherung:

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

Data Sheet (272 KB)

PAR4 antagonist 3 Chemical Structure

CAS. Nr.: 3057206-40-0

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

PAR4

26.1 nM (IC₅₀)

Alle Protease Activated Receptor (PAR) Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Platelet	IC₅₀	26.1 nM Compound: 36	Inhibition of platelet aggregation in human platelet rich plasma preincubated for 5 mins followed by aggregation inducer addition and measured after 5 mins by light transmission aggregometry Inhibition of platelet aggregation in human platelet rich plasma preincubated for 5 mins followed by aggregation inducer addition and measured after 5 mins by light transmission aggregometry	[PMID: 38552183]

In Vitro

PAR4 antagonist 3 (4 μM) exhibits antagonistic effect on GPVI, that inhibits collagen-induced platelet aggregation signaling pathway^[1].

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

In Vivo

PAR4 antagonist 3 (3-12 mg/kg, po, single dose) suppresses the bleeding time, exhibits no impact on the coagulation system in C57BL/J6 mice tail cutting model^[1].
PAR4 antagonist 3 (2 mg/kg, iv or 12 mg/kg, po) shows pharmacokinetics profils as shown in table below:

Pharmacokinetic Analysis of PAR4 antagonist 3 in ICR mice^[1]

Route	Dose (mg/kg)	T_1/2 (h)	T_max (h)	C_max (ng/mL)	AUC_0→t (ng·h/mL)	Cl (mL/h·kg)	F (%)
i.v.	2 mg/kg	11.3	-	-	1250	1428	-
p.o.	12 mg/kg	7.32	1.67	325	3460	-	45

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

Animal Model:

C57BL/J6 mice tail cutting model^[1]
Dosage:

3-12 mg/kg
Administration:

po, single dose
Result:

Suppressed the bleeding time.

Chemical Information

CAS. Nr. 3057206-40-0
Molecular Weight 453.44
Formel C₂₂H₁₆FN₃O₅S
SMILES

FC1=CC=C(OCC2COC3=CC=C4C(OC(C5=CN6C(SC(OC)=N6)=N5)=C4)=C3O2)C=C1
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 (272 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]. Chen P, et al., Discovery of 2,3-Dihydro[1,4]dioxino[2,3-g]benzofuran Derivatives as Protease Activated Receptor 4 (PAR4) Antagonists with Potent Antiplatelet Aggregation Activity and Low Bleeding Tendency. J Med Chem. 2024 Apr 11;67(7):5502-5537. [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.

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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PAR4 antagonist 3

Alle Protease Activated Receptor (PAR) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

PAR4 antagonist 3 Related Classifications

HY-162408 Related Classifications