Apigenin-d₅ 

Apigenin-d5 is a deuterated labeled Apigenin^[1]. Apigenin (4',5,7-Trihydroxyflavone) is a competitive CYP2C9 inhibitor with a K_i of 2 μM.

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]。
Apigenin (4',5,7-Trihydroxyflavone) 抑制细胞色素 P450 2C9 (CYP2C9)，在 CYP2C9 RECO 系统 (一种含有重组人 CYP2C9、P450 的纯化重组酶系统) 中，K_i 为 2 μM还原酶、细胞色素 b₅ 和脂质体)^[2]。Apigenin 抑制细胞增殖。20、40、80 μM的 Apigenin 7d生长抑制率 (IR) 分别为38%、71%、99%。暴露于 Apigenin 24 或 48 小时后，SGC-7901 细胞的克隆形成以剂量和时间依赖性方式受到抑制。Apigenin 处理 24 和 48 h 后 80 μM 的克隆效率分别为 9.8% 和 5%，而对照组为 40.4% 和 43.4%^[3]。

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

Apigenin (4'，5，7-Trihydroxyflavone) 是一种天然类黄酮，具有广泛的生物学特性，包括抗氧化、抗炎、抗癌和神经保护作用。Apigenin (125 mg/kg 和 250 mg/kg) 减轻 Adriamycin (ADR) (24 mg/kg) 诱导的心肌损伤。Apigenin 抑制血清天冬氨酸氨基转移酶 (AST) 的释放。Apigenin 减少血清乳酸脱氢酶 (LDH) 的释放。Apigenin 降低血清肌酸激酶 (CK) 含量^[4]。

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

275.27

C₁₅H₅D₅O₅

263711-74-6

520-36-5

固体

Off-white to light yellow

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [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]. Si D, et al. Mechanism of CYP2C9 inhibition by flavones and flavonols. Drug Metab Dispos. 2009 Mar;37(3):629-34.  [Content Brief]

  [3]. Wu K, et al. Inhibitory effects of apigenin on the growth of gastric carcinoma SGC-7901 cells. World J Gastroenterol. 2005 Aug 7;11(29):4461-4.  [Content Brief]

  [4]. Yu W, et al. Apigenin Attenuates Adriamycin-Induced Cardiomyocyte Apoptosis via the PI3K/AKT/mTOR Pathway. Evid Based Complement Alternat Med. 2017;2017:2590676.  [Content Brief]