MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity.
体外研究
MRS2500 tetraammonium inhibits platelet aggregation to 10 μM ADP with an IC50 of 0.95 nM in human washed platelets. MRS2500 tetraammonium inhibits platelet aggregation to 10μM ADP with an IC50 of 0.49 μM in human PRP.
体内研究
MRS2500 (2 mg/kg; i.v.) decreases acute systemic thromboembolism through selective inhibition of the P2Y1 receptor.
MRS2500 exhibited strong antithrombotic efficacy in the prevention of arterial thrombosis in the monkey ECAT model..
Animal Model:
20-25 g WT Male mice (acute vascular occlusion model)
Dosage:
2 mg/kg
Administration:
Intravenous
Result:
Reduced platelet consumption.
分子式
C13H18N5O8P2I.4[H3N]
分子量
629.28
CAS号
630103-23-0
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.