| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 5g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Ceftriaxone targets bacterial cell wall synthesis by binding to penicillin-binding proteins (PBPs), which are enzymes involved in the final transpeptidation step of peptidoglycan synthesis. This binding inhibits bacterial cell wall formation, leading to cell lysis and death. Ceftriaxone is selectively active against Gram-negative bacteria, including Neisseria gonorrhoeae and Streptococcus pyogenes (MICs = 0.01-0.025 and 0.012-0.25 µg/mL, respectively), over Gram-positive bacteria such as Staphylococcus epidermidis.
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| ln Vitro |
In vitro, ceftriaxone exhibits potent antibacterial activity against a broad spectrum of organisms. It is selectively active against Gram-negative bacteria, including N. gonorrhoeae (MIC = 0.01-0.025 µg/mL) and S. pyogenes (MIC = 0.012-0.25 µg/mL), over Gram-positive bacteria such as S. epidermidis. The compound also demonstrates anti-inflammatory and antioxidant characteristics. Its time-dependent bactericidal activity has been well-characterized.
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| ln Vivo |
In vivo, ceftriaxone is widely used for the treatment of various bacterial infections, including meningitis, pneumonia, sepsis, and gonorrhea. It has a long half-life that allows for once-daily dosing. The compound is administered intravenously or intramuscularly. Its efficacy has been demonstrated in numerous clinical trials, and it is considered a first-line agent for many serious infections, including community-acquired pneumonia and complicated urinary tract infections.
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| Enzyme Assay |
For in vitro susceptibility testing, ceftriaxone is evaluated using standardized broth microdilution or disk diffusion methods according to CLSI or EUCAST guidelines. Bacteria are cultured in appropriate media and incubated with varying concentrations of the compound (typically 0.015-256 µg/mL). The minimum inhibitory concentration (MIC) is determined as the lowest concentration that inhibits visible bacterial growth after 16-24 hours of incubation.
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| Cell Assay |
For in vitro cell-based assays, ceftriaxone is not typically tested on mammalian cell lines, as its primary activity is antibacterial. However, its anti-inflammatory effects can be evaluated on immune cells such as macrophages or peripheral blood mononuclear cells. Cells are treated with the compound at various concentrations (typically 1-100 µg/mL) and stimulated with LPS or other inflammatory stimuli. Cytokine production is measured by ELISA.
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| Animal Protocol |
For in vivo animal experiments, ceftriaxone is typically administered subcutaneously, intravenously, or intramuscularly to mouse or rat models of bacterial infection. Animals are infected with a pathogenic bacterial strain, and treatment is initiated 1-2 hours post-infection. The compound is given at doses ranging from 10-100 mg/kg, typically once or twice daily. Survival rates, bacterial load in tissues, and inflammatory markers are assessed as endpoints.
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| ADME/Pharmacokinetics |
Ceftriaxone has favorable pharmacokinetic properties. It is administered intravenously or intramuscularly with high bioavailability. The drug has a plasma half-life of approximately 5.8-8.7 hours, allowing for once-daily dosing. It is extensively bound to plasma proteins (approximately 85-95%) and is eliminated primarily by renal excretion (approximately 33-67% unchanged in urine) and biliary excretion. The drug penetrates well into tissues and body fluids, including the cerebrospinal fluid.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Limited information suggests that low concentrations of ceftriaxone in breast milk are not expected to have adverse effects on breastfed infants. There are reports that cephalosporins occasionally disrupt the infant's gut microbiota, leading to diarrhea or thrush, but these effects have not been fully assessed. Ceftriaxone is safe for use by breastfeeding women. ◉ Effects on Breastfed Infants A mother exclusively breastfeeding a 52-day-old infant developed a soft tissue infection. She received the following treatment: intravenous teicoplanin 400 mg every 12 hours for 3 days; then 400 mg daily for 5 days; intravenous ceftriaxone 1 g once daily; and topical mupirocin cream twice daily. Careful follow-up examinations showed that her infant did not experience any adverse reactions. ◉ Effects on Lactation and Breast Milk No relevant published information was found as of the revision date. Toxicological data for ceftriaxone indicate that it is generally well-tolerated. Common adverse effects include gastrointestinal disturbances (diarrhea, nausea), injection site reactions, and hypersensitivity reactions (rash, pruritus). Serious adverse effects include anaphylaxis, hemolytic anemia, and biliary sludging. Ceftriaxone is contraindicated in neonates with hyperbilirubinemia due to the risk of bilirubin displacement. It should not be co-administered with calcium-containing solutions due to the risk of precipitation. |
| Additional Infomation |
Ceftriaxone sodium hemihydrate is a cephalosporin. Ceftriaxone sodium is the sodium salt form of ceftriaxone, a β-lactam antibiotic belonging to the third generation of cephalosporins with bactericidal activity. Ceftriaxone binds to and inactivates penicillin-binding protein (PBP) located on the inner membrane of bacterial cell walls. PBP is involved in the final stages of bacterial cell wall assembly and cell wall remodeling during cell division. Inactivation of PBP interferes with the cross-linking of peptidoglycan chains, which is crucial for maintaining the strength and rigidity of bacterial cell walls. This leads to weakening of the bacterial cell wall, ultimately resulting in cell lysis. Compared to second- and first-generation cephalosporins, ceftriaxone has higher activity against Gram-negative bacteria but lower activity against Gram-positive bacteria. Ceftriaxone sodium can also cross the blood-brain barrier and reach therapeutic concentrations in the central nervous system (CNS). It is a broad-spectrum cephalosporin antibiotic, a cefotaxime derivative, with a long half-life and high permeability to the meninges, eyes, and inner ear. See also: ceftriaxone sodium (note moved to).
Ceftriaxone sodium hydrate is a prescription antibiotic approved for the treatment of various bacterial infections. It is marketed under brand names such as Rocephin. The compound is also known as ceftriaxone disodium salt hemiheptahydrate. Its molecular formula is 2C₁₈H₁₆N₈O₇S₃·4Na·7H₂O, and its molecular weight is 1323.19. It is included on the WHO Model List of Essential Medicines. |
| Molecular Formula |
C18H22N8NA2O10S3
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|---|---|
| Molecular Weight |
652.5894
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| Exact Mass |
1322.093
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| CAS # |
104376-79-6
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| Related CAS # |
Ceftriaxone;73384-59-5;Ceftriaxone sodium salt;74578-69-1
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| PubChem CID |
11953897
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| Appearance |
White to off-white solid powder
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| Melting Point |
236ºC
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| Hydrogen Bond Donor Count |
11
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| Hydrogen Bond Acceptor Count |
35
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
83
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| Complexity |
1120
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| Defined Atom Stereocenter Count |
4
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| SMILES |
S1C([H])([H])C(C([H])([H])SC2=NC(C(=NN2C([H])([H])[H])[O-])=O)=C(C(=O)[O-])N2C([C@]([H])([C@@]12[H])N([H])C(/C(/C1=C([H])SC(N([H])[H])=N1)=N\OC([H])([H])[H])=O)=O.[Na+].[Na+].O([H])[H].O([H])[H].O([H])[H]
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| InChi Key |
KTAVBOYXMBQFGR-MAODNAKNSA-J
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| InChi Code |
InChI=1S/2C18H18N8O7S3.4Na.7H2O/c2*1-25-18(22-12(28)13(29)23-25)36-4-6-3-34-15-9(14(30)26(15)10(6)16(31)32)21-11(27)8(24-33-2)7-5-35-17(19)20-7;;;;;;;;;;;/h2*5,9,15H,3-4H2,1-2H3,(H2,19,20)(H,21,27)(H,23,29)(H,31,32);;;;;7*1H2/q;;4*+1;;;;;;;/p-4/b2*24-8-;;;;;;;;;;;/t2*9-,15-;;;;;;;;;;;/m11.........../s1
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| Chemical Name |
tetrasodium;(6R,7R)-7-[[(2Z)-2-(2-amino-1,3-thiazol-4-yl)-2-methoxyiminoacetyl]amino]-3-[(2-methyl-6-oxido-5-oxo-1,2,4-triazin-3-yl)sulfanylmethyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate;heptahydrate
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 | 1.5324 mL | 7.6618 mL | 15.3236 mL | |
| 5 mM | 0.3065 mL | 1.5324 mL | 3.0647 mL | |
| 10 mM | 0.1532 mL | 0.7662 mL | 1.5324 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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