Ceftriaxone-¹³C₂,d₃ triethylammonium salt  (Synonyms: 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]}.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Ceftriaxone (100 μM, 24 h) protects MPP⁺ treated astrocytes by inhibiting the NF-κB/JNK/c-Jun signaling pathway [4].
Ceftriaxone (500 μM, 24-48 h) effectively inhibits unanchored cell growth in A549, H520 and H1650 lung cancer cells by inhibiting Aurora B^[5].

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

Ceftriaxone (200 mg/kg Intraperitoneal injection for 6 weeks) improves functional markers and oxidative stress and inflammation parameters in a rat model of D-galactose (DGL) -induced liver and kidney injury^[6].
Ceftriaxone (200, 400 mg/kg, Intraperitoneal injection) has a protective effect on convulsion induced by Pentylenetetrazol (PTZ) and PTZ-related oxidative damage in rats^[7].
Ceftriaxone (100, 200 mg/kg, Intraperitoneal injection) reduces mechanical dysodynia and hyperalgesia by activating GLT-1 in Streptozocin (HY-13753)-induced diabetic rat models^[8].

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

660.77

C₂₂¹³C₂H₃₀D₃N₉O₇S₃

CN(C(SCC1=C(C(O)=O)N2[C@]([C@H](NC(/C(C3=CS[13C](N)=N3)=N\O[13C]([2H])([2H])[2H])=O)C2=O)([H])SC1)=N4)N=C(O)C4=O.CCN(CC)CC

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]