| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Ceftriaxone targets bacterial penicillin-binding proteins (PBPs), which inhibit bacterial cell wall synthesis. Additionally, ceftriaxone is a covalent inhibitor of GSK3beta (IC₅0=0.78 mM) and an inhibitor of Aurora B.
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| ln Vitro |
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. Studies involving the human use of drugs with labeled deuterium suggest that these compounds may offer some advantages when compared with their nondeuterated counterparts. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs. Deutetrabenazine is the first deuterated drug to receive Food and Drug Administration approval. This deuterated form of the drug tetrabenazine is indicated for the treatment of chorea associated with Huntington's disease as well as tardive dyskinesia. Ongoing clinical trials suggest that a number of other deuterated compounds are being evaluated for the treatment of human diseases and not merely as research tools. [1] Ceftriaxone (100 μM, 24 hours) Protect astrocytes treated with MPP+ by inhibiting the NF-κB/JNK/c-Jun signaling pathway [4]. Ceftriaxone (500 μM, 24-48 h) effectively inhibits the anchorage-independent cell growth of A549, H520, and H1650 lung cancer cells by inhibiting Aurora B[5].
This labeled compound does not have independent in vitro antibacterial activity; its utility lies in its distinct mass for analytical purposes. The non-labeled parent compound ceftriaxone has broad-spectrum antibacterial activity against gram‑negative and gram‑positive bacteria, as well as anti‑inflammatory, antitumor and antioxidant activities. |
| ln Vivo |
Ceftriaxone (200 mg/kg, ip, for 6 weeks) improves functional parameters, as well as oxidative stress and inflammatory parameters in a rat model of liver and kidney injury induced by D-galactose (DGL)[6]. Ceftriaxone (200, 400 mg/kg, ip) protects against pentylenetetrazol (PTZ)-induced seizures and PTZ-related oxidative damage in rats[7]. Ceftriaxone (100, 200 mg/kg, ip) reduces mechanical allodynia and hyperalgesia in a streptozocin (HY-13753)-induced diabetic rat model by activating GLT-1[8].
This compound has no independent in vivo activity as it is a labeled internal standard; however, ceftriaxone (the parent antibiotic) is used to treat bacterial infections including meningitis. |
| Enzyme Assay |
General cell‑free protocol for assessing ceftriaxone binding: A surface plasmon resonance (SPR) assay is used to measure binding of ceftriaxone to penicillin‑binding proteins (PBPs). Recombinant PBP1a, PBP2, or PBP3 is immobilized on a sensor chip, and varying concentrations of ceftriaxone (0.1-100 uM) are flowed over the chip. The association and dissociation rates are measured, and the Kd is calculated.
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| Cell Assay |
Not applicable (Ceftriaxone-¹3C2,d3 triethylammonium salt is not used in cell‑based pharmacological assays).
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| Animal Protocol |
A general animal protocol for assessing the efficacy of the parent compound ceftriaxone: Mice are inoculated intraperitoneally with bacterial pathogens (e.g., E. coli or S. pneumoniae). Ceftriaxone is administered subcutaneously at doses of 50, 100, and 200 mg/kg once or twice daily for 3‑7 days. Survival is monitored daily, and bacterial loads in blood and tissues are quantified by colony‑forming unit (CFU) assays at the end of the study.
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| ADME/Pharmacokinetics |
General PK protocol for the parent compound ceftriaxone: Male Sprague‑Dawley rats are administered ceftriaxone via intravenous (IV, 20 mg/kg) and intramuscular (IM, 40 mg/kg) routes. Blood samples are collected over 24 hours. Plasma concentrations are quantified by LC‑MS/MS using the labeled internal standard. Ceftriaxone has a terminal half‑life of 5‑8 hours in rats and is primarily excreted unchanged in urine.
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| Toxicity/Toxicokinetics |
General toxicity of ceftriaxone has been extensively studied. A 28‑day repeat‑dose IV toxicity study in rats at doses of 100, 500, and 1000 mg/kg/day would be performed. Parameters include clinical signs, body weight, hematology (CBC), serum chemistry (ALT, AST, BUN, creatinine), and histopathology of the kidneys and liver. Ceftriaxone may cause biliary sludge (pseudolithiasis) in the gallbladder at high doses in humans and some animal models.
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| References | |
| Additional Infomation |
Ceftriaxone-¹3C2,d3 triethylammonium salt has the molecular formula C22¹3C2H30D3N₉O₇S3 and a molecular weight of 660.77 g/mol. The compound is typically a solid at room temperature. It serves as a stable isotope-labeled internal standard for quantitative analysis by NMR, GC‑MS, or LC‑MS. The parent compound ceftriaxone was originally developed and marketed by Roche as Rocephin®.
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| Molecular Formula |
C2213C2H30D3N9O7S3
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| Molecular Weight |
660.77
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| Appearance |
Typically exists as solid at room temperature
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| Synonyms |
Ceftriaxone-13C2; Ro 13-9904-13C2,d3 triethylammonium salt
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5134 mL | 7.5669 mL | 15.1339 mL | |
| 5 mM | 0.3027 mL | 1.5134 mL | 3.0268 mL | |
| 10 mM | 0.1513 mL | 0.7567 mL | 1.5134 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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