Prasugrel-¹³C₆  (Synonyms: 普拉格雷-¹³C₆; PCR 4099-¹³C₆)

Prasugrel-13C6 is a deuterated labeled Prasugrel^[1]. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation^[2].

氢、碳和其他元素的稳定重同位素已被纳入药物分子中，主要作为药物开发过程中定量的示踪剂。氘化引起了人们的关注，因为它可能影响药物的药代动力学和代谢谱^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

在大鼠血小板中，Prasugrel 活性代谢物抑制腺苷 ADP (10 μM) 诱导的体外血小板聚集，IC₅₀ 值为 1.8 μM^[3]。
Prasugrel 在体内作用比氯吡格雷更快并且更有效。Prasugrel 是一种无活性的前药，需要在体内进行代谢处理才能产生活性的抗血小板代谢物。Prasugrel 迅速从肠道吸收。口服标准负荷剂量 60 mg 后，活性代谢物的血浆浓度在 1 小时内达到最大值，在 1-2 小时内有效，最大抑制血小板聚集^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

379.40

C₁₄¹³C₆H₂₀FNO₃S

1261394-83-5

150322-43-3

普拉格雷-¹³C₆

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

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

  [3]. 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.  [Content Brief]