PAR4 antagonist 48

Chemical Structure : PAR4 antagonist 48

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货号: PC-21812Not For Human Use, Lab Use Only.

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50 mg		Get quote
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1 g		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	532.55
分子式	C26H21FN6O4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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Solubility	10 mM in DMSO
Chemical Name/SMILES	(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

参考文献

1. Xiaojun Zhang, et al. J Med Chem. 2024 Feb 22. doi: 10.1021/acs.jmedchem.3c01986.