Chemical Structure : PAR4 antagonist 48
CAS No.:
2173201-65-3
PAR4 antagonist 48
Catalog No.: PC-21812Not For Human Use, Lab Use Only.
PAR4 antagonist 48 is a potent and selective quinoxaline-based PAR4 antagonist with IC50 of 1.8 nM in FLIPR calcium mobilization assays, inhibits calcium mobilization in human platelet-rich plasma (PRP) aggregation assay with γ-thrombin with IC50 of 2.1 nM.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
PAR4 antagonist 48 is a potent and selective quinoxaline-based PAR4 antagonist with IC50 of 1.8 nM in FLIPR calcium mobilization assays, inhibits calcium mobilization in human platelet-rich plasma (PRP) aggregation assay with γ-thrombin with IC50 of 2.1 nM.
PAR4 antagonist 48 is equally potent to BMS-986120 (Cat# PC-60548).
PAR4 antagonist 48 displays excellent selectivity versus PAR1 (PAR1 FLIPR IC50 > 5 μM), does not show significant issues with CYP inhibition, PXR activation, and ion channel inhibitions.
PAR4 antagonist 48 inhibits in vitro whole blood platelet aggregation in monkeys with an IC80 value of 3.6 nM.
PAR4 antagonist 48 does not exhibit ex vivo platelet aggregation response to PAR1 AP, collagen, or ADP.
PAR4 antagonist 48 (3 mg/kg oral) exhibits antithrombotic efficacy in the monkey electrically induced carotid arterial thrombosis (ECAT) model.
Physicochemical Properties
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M.Wt
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532.55
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Formula
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C26H21FN6O4S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(R)-(5-Fluoro-2-(2-methoxy-7-methylquinoxalin-5-yl)-7,8-dihydrobenzofuro[5,4-d]thiazol-7-yl)methyl (2-methylpyrimidin-5-yl)carbamate
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References
1. Xiaojun Zhang, et al. J Med Chem. 2024 Feb 22. doi: 10.1021/acs.jmedchem.3c01986.
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