| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Ceftaroline targets the penicillin-binding proteins (PBPs), specifically PBP2a in methicillin-resistant Staphylococcus aureus (MRSA) and PBP2x in Streptococcus pneumoniae. It is a beta-lactam antibiotic that inhibits bacterial cell wall synthesis by binding to these PBPs, which are transpeptidases that cross-link the peptidoglycan polymer. This leads to the weakening of the cell wall, osmotic lysis, and bacterial cell death. Ceftaroline hydrochloride is a broad-spectrum cephalosporin with activity against Gram-positive and Gram-negative bacteria.
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| ln Vitro |
Ceftaroline hydrochloride exhibits potent in vitro activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and Streptococcus pneumoniae. The minimum inhibitory concentration (MIC₅0) for MRSA is typically 0.5-1 ug/mL. It also has activity against some Gram-negative organisms, such as Haemophilus influenzae. Ceftaroline is active against Enterobacteriaceae, but resistance can occur. The compound is not cytotoxic to human cells at therapeutic concentrations. It is a reference standard for antimicrobial susceptibility testing.
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| ln Vivo |
In vivo, ceftaroline fosamil is the parenteral prodrug that is rapidly hydrolyzed to the active ceftaroline after intravenous administration. The drug is approved for the treatment of acute bacterial skin and skin structure infections (ABSSSI) at a dose of 600 mg IV every 12 hours for 5-14 days. In a mouse model of septicemia, ceftaroline (2-10 mg/kg, IV) protected mice from lethal infection by MRSA and S. pneumoniae. The in vivo efficacy correlates with the time above the MIC (T > MIC). It is also effective against community-acquired pneumonia.
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| Enzyme Assay |
Ceftaroline hydrochloride is not an enzyme inhibitor; it is a PBP binding agent. The binding affinity to PBPs is measured by competitive binding assays using fluorescently labeled penicillin. The IC₅0 for the inhibition of PBP2a from MRSA is in the low ug/mL range. For research use, the compound is used as a reference standard for HPLC. The purity is >98.5%.
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| Cell Assay |
For antimicrobial susceptibility testing, the minimum inhibitory concentration (MIC) is determined by the broth microdilution method according to CLSI guidelines. Bacteria are cultured in cation-adjusted Mueller-Hinton broth (CAMHB) to 5×10⁵ CFU/mL. Ceftaroline hydrochloride is serially diluted 2-fold (0.03-64 ug/mL) in 96-well plates. Plates are incubated at 35degC for 18-24 h. The MIC is the lowest concentration with no visible growth. For cytotoxicity, HepG2 cells are treated with ceftaroline (1-1000 ug/mL) for 24 h, and cell viability is measured by MTT assay. The CC₅0 is >500 ug/mL.
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| Animal Protocol |
In the neutropenic mouse thigh infection model, female ICR mice (20-25 g, n=5/group) are rendered neutropenic by cyclophosphamide (150 mg/kg, IP) at 4 days and 1 day before infection. The mice are infected intramuscularly with 10⁶ CFU of MRSA (e.g., ATCC 43300). Ceftaroline hydrochloride is dissolved in saline and administered subcutaneously (SC) at 2, 4, 8, 16, 32 mg/kg at 2 h post-infection. After 24 h, mice are euthanized, and the thigh muscles are harvested, homogenized, and plated for CFU enumeration. The change in log10 CFU/thigh is calculated. The dose required to achieve a 1-log reduction is determined.
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| ADME/Pharmacokinetics |
Ceftaroline fosamil (prodrug) has a half-life of approximately 1.6 hours in humans. Ceftaroline is primarily excreted unchanged in the urine. The volume of distribution is approximately 20 L. Protein binding is low (<20%). After intravenous administration of 600 mg ceftaroline fosamil, the peak plasma concentration (Cmax) of ceftaroline is approximately 20-30 ug/mL. The compound is not metabolized by CYP450 enzymes. The pharmacokinetics are linear. No food effect.
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| Toxicity/Toxicokinetics |
Ceftaroline hydrochloride is generally well-tolerated. The most common adverse reactions in clinical trials are diarrhea (7%), nausea (6%), and headache (5%). Less common but serious adverse effects include seizures (especially in patients with renal impairment) and hypersensitivity reactions (including anaphylaxis and Stevens-Johnson syndrome). It is contraindicated in patients with a history of severe hypersensitivity to cephalosporins. As a beta-lactam, it can cause cross-reactivity with penicillins.
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| References |
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| Additional Infomation |
Ceftaroline hydrochloride is a research-grade beta-lactam antibiotic standard. It is not an FDA-approved drug for human use as a single entity; the prodrug ceftaroline fosamil (Teflaro) is approved. Ceftaroline hydrochloride is used for impurity profiling and quality control (QC) of ceftaroline fosamil drug substance and for in vitro antimicrobial susceptibility testing. For research use only, not for diagnostic or therapeutic applications.
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| Molecular Formula |
C22H21CLN8O5S4
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|---|---|
| Molecular Weight |
641.17
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| Related CAS # |
189345-04-8 Ceftaroline
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| Appearance |
Light yellow to yellow solid powder
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| Synonyms |
Cefuroxime hydrochloride; Cefuroxime HCl; T-91825 hydrochloride; T-91825 HCl; T91825 hydrochloride; T91825 HCl
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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 | 1.5596 mL | 7.7982 mL | 15.5965 mL | |
| 5 mM | 0.3119 mL | 1.5596 mL | 3.1193 mL | |
| 10 mM | 0.1560 mL | 0.7798 mL | 1.5596 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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