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 T1/2 of 97.6 min.
For research use only. We do not sell to patients.
- CAS No.: 3057206-40-0
- Formula: C22H16FN3O5S
- Molecular Weight:453.44
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PAR4 26.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| Platelet | IC50 |
26.1 nM
Compound: 36
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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
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[PMID: 38552183] |
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.
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) | T1/2 (h) | Tmax (h) | Cmax (ng/mL) | AUC0→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.
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Animal Model:C57BL/J6 mice tail cutting model[1]
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Dosage:3-12 mg/kg
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Administration:po, single dose
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Result:Suppressed the bleeding time.
Chemical Information
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CAS No. 3057206-40-0
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Molecular Weight 453.44
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Formula C22H16FN3O5S
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SMILES
FC1=CC=C(OCC2COC3=CC=C4C(OC(C5=CN6C(SC(OC)=N6)=N5)=C4)=C3O2)C=C1
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAR4 antagonist 3 Related Classifications
HY-162408 Related Classifications
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