Bioactivity | PAR4 antagonist 4 (Compound 37) is a selective antagonist for protease activated receptor 4 (PAR4). PAR4 antagonist 3 exhibits antiplatelet efficacy with IC50 of 14.2 nM. PAR4 antagonist 3 improves metabolic stablility in human liver microsomes with T1/2 of 42.5 min[1]. |
Invitro | PAR4 antagonist 4 (4 μM) 对 GPVI 具有拮抗作用,抑制胶原诱导的血小板聚集信号通路[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PAR4 antagonist 4 相关抗体: |
In Vivo | PAR4 antagonist 4 (3-12 mg/kg,口服,单剂量) 抑制 C57BL/J6 小鼠切尾模型出血时间,对凝血系统无影响[1]。PAR4 antagonist 4 (2 mg/kg,静脉注射或 12 mg/kg,口服) 具有如表格所示的药代动力学特性:Pharmacokinetic Analysis of PAR4 antagonist 4 in ICR mice[1]Route |
Formula | C22H16FN3O5S |
Molar Mass | 453.44 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |