| Bioactivity | PAR4 antagonist 7 (Compound 20f) is selective PAR4 antagonist (IC50: 1.72 nM). PAR4 antagonist 7 inhibits PAR4 agonist-induced platelet aggregation. PAR4 antagonist 7 has good metabolic stability. PAR4 antagonist 7 does not show a bleeding tendency in mice[1]. |
| Invitro | PAR4 antagonist 7 抑制 PAR4 激动剂肽 (PAR4-AP) (75 μM) 诱导的洗涤血小板 (WP) 聚集，IC50 为 15.32 nM[1]。PAR4 antagonist 7 抑制 PAR4-AP (75 μM) 诱导的人富含血小板的血浆 (PRP) 水平，IC50 为 6.39 nM[1]。PAR4 antagonist 7 还抑制 AYPGKF-NH2 (75 μM) 或凝血酶 (0.1 U/mL) 诱导的人类 PRP 血小板聚集，并且不影响 SFLLRN-NH2 (5 μM)、胶原蛋白 (10 mg/mL)、ADP (10 μM) 或U46619 (HY-108566) (3 μM) 诱导血小板聚集[1]。PAR4 antagonist 7 在人肝微粒体中表现出优异的代谢稳定性 (T1/2 = 249.83 分钟)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> PAR4 antagonist 7 相关抗体: |
| In Vivo | PAR4 antagonist 7 (2.5-10 mg/kg，灌胃) 在小鼠中没有表现出出血倾向，有解决出血风险的潜力[1]。PAR4 antagonist 7 在大鼠中的药代动力学特性 (Compound 20f)Dose (mg/kg) |
| Formula | C28H20FN5O4S |
| Molar Mass | 541.55 |
| 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]. Li S, et al. Discovery of quinazoline-benzothiazole derivatives as novel potent protease-activated receptor 4 antagonists with improved pharmacokinetics and low bleeding liability. Eur J Med Chem. 2024 Dec 15;280:116980. |