MRS2500 tetraammonium

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CAS NO:

630103-23-0

MRS2500 tetraammonium 是一种高效、选择性和稳定的P2Y1受体拮抗剂 (K_i=0.78 nM)。MRS2500 tetraammonium 抑制 ADP 诱导的人血小板聚集，IC₅₀值为 0.95 nM。具有抗血栓活性。

生物活性

MRS2500 tetraammonium is a potent, selective and stable antagonist of theP2Y1receptor (K_i=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC₅₀value of 0.95 nM. Antithrombotic activity^[1]^[2]^[3].

体外研究
(In Vitro)

MRS2500 tetraammonium inhibits platelet aggregation to 10 μM ADP with an IC₅₀of 0.95 nM in human washed platelets. MRS2500 tetraammonium inhibits platelet aggregation to 10μM ADP with an IC₅₀of 0.49 μM in human PRP^[4].

体内研究
(In Vivo)

MRS2500 (2 mg/kg; i.v.) decreases acute systemic thromboembolism through selective inhibition of the P2Y1 receptor^[3].
MRS2500 exhibited strong antithrombotic efficacy in the prevention of arterial thrombosis in the monkey ECAT model^[4]..

Animal Model:	20-25 g WT Male mice (acute vascular occlusion model)^[3]
Dosage:	2 mg/kg
Administration:	Intravenous
Result:	Reduced platelet consumption.

分子量

629.28

性状

Solid

Formula

C₁₃H₃₀IN₉O₈P₂

CAS 号

630103-23-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)