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Prasugrel

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Chemical Structure| 150322-43-3 同义名 : PCR 4099;CS 747;LY640315
CAS号 : 150322-43-3
货号 : A125835
分子式 : C20H20FNO3S
纯度 : 98%
分子量 : 373.441
MDL号 : MFCD09954140
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(281.17 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+30% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

生物活性
靶点

  • P2Y receptor
描述 The platelet P2Y12 receptor (P2Y12R) for adenosine 5'diphosphate (ADP) plays a central role in platelet function, hemostasis, and thrombosis [3].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. 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 1-2h [4]. Oral administration of prasugrel to rats resulted in dose-related and time-related inhibition of ex vivo platelet aggregation, and its effect was about 10 times more potent than that of clopidogrel. In rat platelets, prasugrel AM inhibited in vitro platelet aggregation induced by adenosine 5'-diphosphate (ADP) (10 microm) with an IC(50) value of 1.8 microm[5]. Post-administration of prasugrel for 3 and 5 days reduced neurological deficit scores and improved the spontaneous activity/short term spatial memory using the Y-maze paradigm. On the molecular level, prasugrel turned off SUMO2/3-inhibitory kappa (Iκ)Bα, Ubc9 and nuclear factor kappa (NF-κ)B. Besides, it inhibited malondialdehyde (MDA) and inactivated astrocytes by downregulating the glial fibrillary acidic protein (GFAP) hippocampal immune-expression[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.68mL

0.54mL

0.27mL

13.39mL

2.68mL

1.34mL

26.78mL

5.36mL

2.68mL
参考文献

[1]Schror K, Siller-Matula JM, et al. Pharmacokinetic basis of the antiplatelet action of prasugrel. Fundam Clin Pharmacol. 2012 Feb;26(1):39-46.

[2]Darius H. [Prasugrel] . Hamostaseologie. 2012;32(3):186-90.

[3]M Cattaneo, P2Y12 receptors: structure and function. J Thromb Haemost. 2015 Jun;13 Suppl 1:S10-6.

[4]Wijeyeratne YD, et al. Anti-platelet therapy: ADP receptor antagonists. Br J Clin Pharmacol. 2011 Oct;72(4):647-57.

[5] 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 clopidogrel's active metabolite. J Thromb Haemost. 2007 Jul;5(7):1545-51.

[6] Asmaa A Gomaa, Hanan S El-Abhar, et al. Prasugrel anti-ischemic effect in rats: Modulation of hippocampal SUMO2/3-IкBα/Ubc9 and SIRT-1/miR-22 trajectories. Toxicol Appl Pharmacol. 2021 Sep 1;426:115635.