Exemestane-¹³C,d₂  (Synonyms: 依西美坦-¹³C,d₂; FCE 24304-¹³C,d₂; EXE-¹³C,d₂)

Exemestane-¹³C,d₂ is ¹³C and deuterated labeled Exemestane (HY-13632). Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC₅₀s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research^[1][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]。
Exemestane (1-1000 nM；72 h；hFOB，Saos-2 细胞) 显著增加细胞数量^[3]。
Exemestane (72 h) 增加 hFOB 和 Saos-2 细胞中的碱性磷酸酶活性，并诱导 hFOB 细胞中 MYBL2、OSTM1、HOXD11、ADCYAP1R1 和磷脂酰肌醇蛋白聚糖 2 的表达^[3]。
Exemestane 竞争性抑制和时间依赖性地灭活人胎盘芳香酶，K_i 为 4.3 nM。Exemestane 取代大鼠前列腺雄激素受体中的 [³H]5α-dihydrotestosterone，IC₅₀ 为 0.9 μM^[2]。

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

Exemestane (20-100 mg/kg；肌肉注射；每周一次；持续 16 周) 处理显著增加腰椎和股骨 BMD、股骨弯曲强度、第五腰椎抗压强度和骨小梁体积。Exemestane 显著降低卵巢切除术引起的血清吡啶啉和血清骨钙素的增加。Exemestane 显著降低血清胆固醇和低密度脂蛋白胆固醇^[4]。
Exemestane (20 mg/kg/天皮下注射) 诱导 26% 的完全 (CR) 和 18% 的部分 (PR) 大鼠体内 7，12-二甲基苯并蒽 (DMBA) 诱导的乳腺肿瘤肿瘤消退^[5]。

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

299.41

C₁₉¹³CH₂₂D₂O₂

依西美坦-¹³C,d₂

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]. Di Salle, E., et al., Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol, 1994. 49(4-6): p. 289-94.  [Content Brief]

  [3]. Miki, Y, et al. Effects of aromatase inhibitors on human osteoblast and osteoblast-like cells: a possible androgenic bone protective effects induced by exemestane. Bone. 2004 Sep 1;10(17):5717-23.  [Content Brief]

  [4]. Goss, P.E., et al., Effects of the steroidal aromatase inhibitor exemestane and the nonsteroidal aromatase inhibitor letrozole on bone and lipid metabolism in ovariectomized rats. Clin Cancer Res, 2004. 10(17): p. 5717-23.  [Content Brief]

  [5]. Zaccheo, T., D. Giudici, and E. Di Salle, Inhibitory effect of combined treatment with the aromatase inhibitor exemestane and tamoxifen on DMBA-induced mammary tumors in rats. J Steroid Biochem Mol Biol, 1993. 44(4-6): p. 677-80.  [Content Brief]