Ceftriaxone-¹³C₂,d₃ triethylammonium salt  (Synonyms: 头孢曲松-¹³C₂; Ro 13-9904-¹³C₂,d₃ triethylammonium salt)

Ceftriaxone-¹³C₂,d₃ triethylammonium salt is ¹³C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC₅₀ value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis^{[1][2][3][4][5][6][7]}.

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]。
Ceftriaxone (100 μM, 24 h) 通过抑制 NF-κB /JNK/c-Jun 信号通路保护被 MPP⁺ 处理的星形细胞^[4]。
Ceftriaxone (500 μM, 24-48 h) 通过抑制极光激酶 B (Aurora B) 有效抑制 A549、H520 和H1650 肺癌细胞的非锚定细胞生长^[5]。

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

Ceftriaxone (200 mg/kg, 腹腔注射, 连续 6 周) 在 D-半乳糖 (DGL) 诱导的大鼠肝肾损伤模型中可改善功能指标，以及氧化应激和炎症参数^[6]。
Ceftriaxone (200, 400 mg/kg, 腹腔注射) 对大鼠 Pentylenetetrazol (PTZ) 致惊厥及PTZ 相关氧化损伤具有保护作用^[7]。
Ceftriaxone (100, 200 mg/kg, 腹腔注射) 在 Streptozocin (HY-13753) 诱导的糖尿病大鼠模型中通过激活 GLT-1 减少机械性异常性痛和痛觉过敏^[8]。

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

660.77

C₂₂¹³C₂H₃₀D₃N₉O₇S₃

73384-59-5

头孢曲松-¹³C₂；头孢三嗪-¹³C₂

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]. Nahata MC, et al. Ceftriaxone: a third-generation cephalosporin. Drug Intell Clin Pharm. 1985 Dec;19(12):900-6.  [Content Brief]

  [3]. Nassar H, et al. Molecular docking, molecular dynamics simulations and in vitro screening reveal cefixime and ceftriaxone as GSK3β covalent inhibitors. RSC Adv. 2023 Apr 11;13(17):11278-11290.  [Content Brief]

  [4]. Zhang Y, et al. Ceftriaxone Protects Astrocytes from MPP(+) via Suppression of NF-κB/JNK/c-Jun Signaling. Mol Neurobiol. 2015 Aug;52(1):78-92.  [Content Brief]

  [5]. Li X, et al. Ceftriaxone, an FDA-approved cephalosporin antibiotic, suppresses lung cancer growth by targeting Aurora B. Carcinogenesis. 2012 Dec;33(12):2548-57.  [Content Brief]

  [6]. Hakimizadeh E, et al. Ceftriaxone improves hepatorenal damages in mice subjected to D-galactose-induced aging. Life Sci. 2020 Oct 1;258:118119.  [Content Brief]

  [7]. Uyanikgil Y, et al. Positive effects of ceftriaxone on pentylenetetrazol-induced convulsion model in rats. Int J Neurosci. 2016;126(1):70-5.  [Content Brief]

  [8]. Gunduz O, et al. Anti-allodynic and anti-hyperalgesic effects of ceftriaxone in streptozocin-induced diabetic rats. Neurosci Lett. 2011 Mar 10;491(1):23-5.  [Content Brief]