Ceftriaxone |
Catalog No.GC35648
One-Click Copy Product Info
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Ceftriaxone is a β -lactam antibiotic with broad-spectrum bactericidal activity, which has good antibacterial activity against a variety of Gram-negative and Gram-positive bacteria.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 73384-59-5
Sample solution is provided at 25 µL, 10mM.
Ceftriaxone is a β -lactam antibiotic with broad-spectrum bactericidal activity, which has good antibacterial activity against a variety of Gram-negative and Gram-positive bacteria. Ceftriaxone is used for a variety of infections such as community-acquired pneumonia, meningitis and gonorrhea. Ceftriaxone is a covalent inhibitor of Glycogen Synthase Kinase 3β (GSK3β), with an IC50 value of 0.78μM under the condition of 60 minutes preincubation. GSK3β is a serine/threonine kinase that has been suggested as a putative drug target for several diseases. In cancer, Ceftriaxone excerts antiproliferative, cell cycle arresting and apoptosis induction properties; in Alzheimer's Disease (AD), Ceftriaxone decreases amyloid-β peptide production and upregulate glutamate transporter-1 mediated by the inhibition of tau hyperphosphorylation[1][2].
In vitro, treatment with 500-1000μM Ceftriaxone for 10 days (A549), 7 days (H520), or 14 days (H1650) resulted in a significant and dose-dependent reduction in colony formation by targeting Aurora B[2]. Ceftriaxone (100μg/mL; 3h) upregulated NOD-like receptor family pyrin domain containing 3 (NLRP3) and pro-caspase-1 transcription but attenuated NLRP3 protein expression in LPS-induced A549 and PC3 cells[4].
In vivo, Ceftriaxone (100mg/kg; i.p.; three times a week) significantly slowed tumor growth and reduced tumor size in athymic nude mice bearing A549 (57d) or H520 (32d) xenografts by inhibiting Aurora B activity[2]. Ceftriaxone (200mg/kg/d; i.p.; 6w) improved functional indicators, oxidative stress, and inflammatory parameters in the D-galactose (DGL)-induced liver and kidney injury rat model[3].
References:
[1] Nassar H, Sippl W, Dahab RA, Taha M. Molecular docking, molecular dynamics simulations and in vitro screening reveal cefixime and ceftriaxone as GSK3β covalent inhibitors. RSC Adv. 2023;13(17):11278-11290.
[2] Li X, Li H, Li S, et al. Ceftriaxone, an FDA-approved cephalosporin antibiotic, suppresses lung cancer growth by targeting Aurora B. Carcinogenesis. 2012;33(12):2548-2557.
[3] Hakimizadeh E, et al. Ceftriaxone improves hepatorenal damages in mice subjected to D-galactose-induced aging. Life Sci. 2020 Oct 1;258:118119.
[4] Tezcan G, Alsaadi M, Hamza S, Garanina EE, Martynova EV, Ziganshina GR, Farukshina ER, Rizvanov AA, Khaiboullina SF. Azithromycin and Ceftriaxone Differentially Activate NLRP3 in LPS Primed Cancer Cells. International Journal of Molecular Sciences. 2022; 23(16):9484.
| Kinase experiment [1]: | |
Preparation Method | Ceftriaxone was dissolved in 100% (v/v) DMSO to form a 10mM stock solution (2ml). Ceftriaxone was initially screened at 100μM against GSK3β. The bioassay was conducted in black 384-well plates. For testing Ceftriaxone, 100nl of the stock solution (10mM) was mixed with 5μl of the peptide/kinase mixture, 2.4μl of the kinase buffer (50mM HEPES pH 7.5, 0.01% BRIJ-35, 10mM MgCl2, 1mM EGTA) and 2.5μl of the ATP solution. The final 10μl kinase reaction included the tested cephalosporin concentration (100μM), 1% (v/v) DMSO, kinase peptide substrate and 25μM ATP in 50mM HEPES pH 7.5, 0.01% BRIJ-35,10mM MgCl2, and 1mM EGTA. The mixture was shaken for 30s then incubated at room temperature for 60min to complete the kinase reaction. Subsequently, 5μl of the development reagent solution was added to each reaction mixture, shaken for 30s and left for another 60min at room temperature. Ultimately, fluorescence emissions were measured at λex of 445 and λem of 520nm. To assess the potential of Ceftriaxone to irreversibly inhibit GSK3β, it was initially incubated at 10μM with the kinase for 60min before adding the ATP solution. |
Reaction Conditions | 100μM; 30s+60min or 60min+60min |
Applications | Ceftriaxone resulted in more than 60% inhibition and were considered for further screening to calculate its IC50 value. The IC50 value for GSK3β without preincubation is 7.35μM. After 60 minutes preincubation with GSK3β, the IC50 value decreased to 0.78μM. |
| Cell experiment [2]: | |
Cell lines | A549, H520 and H1650 cells |
Preparation Method | Cells were cultured with different concentrations of Ceftriaxone for 10 days (A549), 7 days (H520) or 14 days (H1650) and then colonies were counted. |
Reaction Conditions | 500 or 1000μM; 7, 10 or 14d |
Applications | A549, H520 or H1650 cells treated with Ceftriaxone had a significant reduction in colony formation compared with untreated control cells. |
| Animal experiment [2]: | |
Animal models | Athymic nude mice (Cr:NIH(S), NIH Swiss nude, 6–9 weeks old) |
Preparation Method | Mice were randomly divided into three groups: (i) vehicle group; (ii) 100mg/kg Ceftriaxone-treated group; (iii) no cells-injected group. Treated with 100mg/kg Ceftriaxone A549 or H520 cells were inoculated subcutaneously (2×106 cells) into the left flank of each mouse in the first two groups. Treatment was started when the tumors reached a mean tumor volume of 100mm3. For the Ceftriaxone group, 2.5mg Ceftriaxone, formulated in 500µl physiological saline, was administered to each mouse three times per week by intraperitoneal (i.p.) injection. For the vehicle group, 500µl physiological saline was administered to each mouse three times per week by i.p. injection. The duration of the animal study was 57 days for A549 cells and 32 days for H520 cells. |
Dosage form | 100mg/kg; 3 times a week; i.p. |
Applications | The tumors treated with 100mg/kg Ceftriaxone grew significantly more slowly and the sizes of the tumors were smaller compared with the vehicle group. Expression of phosphorylated histone H3 was substantially decreased in the ceftriaxone-treated group compared with the vehicle group. Ceftriaxone suppressed tumor growth by inhibiting Aurora B activity in vivo. |
References: | |
| Cas No. | 73384-59-5 | SDF | |
| Canonical SMILES | O=C(C(N12)=C(CSC(N(C)NC3=O)=NC3=O)CS[C@]2([H])[C@H](NC(/C(C4=CSC(N)=N4)=N\OC)=O)C1=O)O | ||
| Formula | C18H18N8O7S3 | M.Wt | 554.58 |
| Solubility | DMSO:≥100mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8032 mL | 9.0158 mL | 18.0317 mL |
| 5 mM | 360.6 μL | 1.8032 mL | 3.6063 mL |
| 10 mM | 180.3 μL | 901.6 μL | 1.8032 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)