Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation.
性状
Solid
IC50 & Target[1][2]
P2Y12 receptor
体内研究(In Vivo)
In rat platelets, Prasugrel active metabolite inhibits in vitro platelet aggregation induced by adenosine ADP (10μM) with an IC 50 value of 1.8 μM.
Prasugrel acts faster and is significantly more potent than Clopidogrel in vivo. Prasugrel is an inactive prodrug that requires metabolic processing in vivo to generate the active antiplatelet metabolite. Prasugrel is rapidly absorbed from the gut. After oral administration of standard-loading doses of 60 mg, maximum plasma levels of the active metabolite are achieved within 1 h, effective, maximum inhibition of platelet aggregation at 1-2 h. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Wijeyeratne YD, et al. Anti-platelet therapy: ADP receptor antagonists. Br J Clin Pharmacol. 2011 Oct;72(4):647-57.[2]. Sugidachi A, et al. The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrels active metabolite. J Thromb Haemost
溶解度数据
In Vitro: DMSO : 100 mg/mL (267.78 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液