Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease.
体外研究
Atopaxar (0.0001-10 μM; 1h) inhibits haTRAP (high-affinity thrombin receptor activating peptide) binding to PAR-1 on human platelet membranes in a concentration-dependent manner, with an IC50 of 0.019 μM.
Atopaxar inhibits human platelet aggregation induced by thrombin or TRAP in a concentration-dependent manner.
Atopaxar does not inhibit PRP (platelet-rich plasma) aggregation induced by ADP, U46619, collagen, and PAR-4ap, up to a concentration of 20 μM.
体内研究
Atopaxar (30-100 mg/kg; p.o.) causes a dose-dependent prolongation of the time to occlusion of the femoral artery in photochemically-induced thrombosis (PIT) guinea pigs model.
Atopaxar does not prolong bleeding time in guinea pigs at the highest tested dosage of 1000 mg/kg.
Animal Model:
Guinea pigs, PIT model
Dosage:
Oral administration
Administration:
10 mg/kg, 30 mg/kg, 100 mg/kg
Result:
Prolonged the time to occlusion by 1.8-fold and 2.4-fold at 30 mg/kg and 100 mg/kg, respectively, compared with controls.
分子式
C29H38N3O5F.HBr
分子量
527.63
CAS号
751475-53-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Please store the product under the recommended conditions in the Certificate of Analysis.
溶解性数据
In Vitro:
DMSO : 250 mg/mL (473.82 mM; Need ultrasonic)
配制储备液
浓度溶剂体积质量
1 mg
5 mg
10 mg
1 mM
1.8953 mL
9.4763 mL
18.9527 mL
5 mM
0.3791 mL
1.8953 mL
3.7905 mL
10 mM
0.1895 mL
0.9476 mL
1.8953 mL
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: