Ceftaroline
Based on 1 publication(s) in Google Scholar
Ceftaroline (T-91825) is a cephalosporin compound and the active form of Ceftaroline fosamil (HY-14737). Ceftaroline exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and some anaerobic bacteria. Ceftaroline binds to penicillin-binding proteins 2 and 2A, thereby inhibiting the synthesis of bacterial peptidoglycan and cell wall, and acts as a bactericide, synergist, and resistance inhibitor. Ceftaroline can be used in research related to complicated skin and soft tissue infections, community-acquired pneumonia, Enterococcus faecalis infective endocarditis, and bacterial infections.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.0%
- CAS. Nr.: 189345-04-8
- Formel: C22H20N8O5S4
- Molecular Weight:604.70
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Speicherung:
-80°C, stored under nitrogen
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ceftaroline
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Biologische Aktivität
Beschreibung
In Vitro
Ceftaroline (T-91825) in combination with Daptomycin (HY-B0108) exhibits synergistic in vitro activity against all tested endocarditis-associated HLAR and non-HLAR Enterococcus faecalis isolates at standard initial inoculum, prevents daptomycin resistance development, and shows bactericidal activity against two HLAR strains[2].
Ceftaroline (1/4-4 MIC; 6-24 h) exhibits rapid, potent bactericidal activity against MRSA strains OFU4 and TY6242 at concentrations of 2 MIC and higher, reducing viable cell counts significantly over 24 h[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Ceftaroline, delivered via its prodrug TAK-599 (20 mg/kg; s.c.; three times daily; starting 2 hours post infection or day 1 and day 2 post infection), significantly reduces MRSA bacterial counts in the lungs of neutropenic mice, even when treatment is initiated at a late stage of infection[4].
Ceftaroline, delivered via its prodrug TAK-599 (20 mg/kg; s.c.; three doses; at 2, 20, and 26 hours post infection), reduces MRSA bacterial counts in mouse thigh muscle to 0.1% or less of control levels[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ICR mice (4-week-old male; systemic MRSA infection model via intraperitoneal MRSA injection in 5% mucin)[4]
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Dosage:1.08 mg/kg (strain TY5826); 1.46 mg/kg (strain TY6007); 4.81 mg/kg (strain TY5993); 2.09 mg/kg (strain TY6242)
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Administration:s.c.; single dose; 1 hour post bacterial challenge
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Result:Achieved ED50 of 1.08 mg/kg for protection against systemic MRSA infection (strain TY5826).
Achieved ED50 of 1.46 mg/kg for protection against systemic MRSA infection (strain TY6007).
Achieved ED50 of 4.81 mg/kg for protection against systemic MRSA infection (strain TY5993).
Achieved ED50 of 2.09 mg/kg for protection against systemic MRSA infection (strain TY6242).
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Animal Model:CBA/J mice (5-week-old female; neutropenic MRSA pneumonia model via intranasal MRSA inoculation, neutropenia induced by intraperitoneal cyclophosphamide 4 days and 1 day pre-infection)[4]
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Dosage:20 mg/kg
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Administration:s.c.; three times daily; starting 2 hours post infection or day 1 and day 2 post infection
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Result:Reduced lung bacterial counts by more than 99.9% compared to untreated day 3 controls when treatment started on day 1 after infection.
Reduced lung bacterial counts to 1/100 the level of day 1 controls when treatment started on day 1 after infection.
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Animal Model:ICR mice (4-week-old male; MRSA thigh muscle infection model via intramuscular MRSA injection in left thigh)[4]
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Dosage:20 mg/kg
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Administration:s.c.; three doses; at 2, 20, and 26 hours post infection
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Result:Reduced thigh muscle bacterial counts to 0.1% or less of untreated control levels.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 189345-04-8
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Appearance Solid
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Molecular Weight 604.70
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Formel C22H20N8O5S4
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Color White to yellow
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SMILES
C[N+]1=CC=C(C2=CSC(SC(CS[C@]3([H])[C@@H]4NC(/C(C5=NSC(N)=N5)=N\OCC)=O)=C(C([O-])=O)N3C4=O)=N2)C=C1
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Synonyms
T-91825; PPI-0903M
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Versand
Shipping with dry ice.
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Speicherung
-80°C, stored under nitrogen
Publications (1)
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Journal Impact Factor
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Most Recent
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J Infect Dis
Enhanced Killing of Methicillin-Resistant Staphylococcus aureus With Ceftaroline or Vancomycin in Combination With Carbapenems. [Abstract]2025 Jul 30;232(1):181-190. PMID: 39777519
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (165.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1.82 mg/mL (3.01 mM; ultrasonic and warming and heat to 60°C)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Anaerobic Bacterial Culture
Anaerobic bacterial culture detects viable bacteria that can grow under oxygen-depleted conditions; the readout is visible colony formation or broth turbidity after incubation in a chamber, jar, pouch, bag, or roll-tube system that maintains anaerobiosis. Oxygen control is central to the method because recovery depends on limiting oxygen exposure during collection, transport, inoculation, and incubation.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
Reinheit & Dokumentation
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Data Sheet (292 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[3]. Sader HS, et al. Antimicrobial activity and spectrum of PPI-0903M (T-91825), a novel cephalosporin, tested against a worldwide collection of clinical strains. Antimicrobial agents and chemotherapy. 2005 Aug;49(8):3501-12. [Content Brief]
[4]. Iizawa Y, et al. In vitro antimicrobial activity of T-91825, a novel anti-MRSA cephalosporin, and in vivo anti-MRSA activity of its prodrug, TAK-599. Journal of infection and chemotherapy : official journal of the Japan Society of Chemotherapy. 2004 Jun;10(3):146-56. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months (stored under nitrogen). When stored at -80°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 1.6537 mL | 8.2686 mL | 16.5371 mL | 41.3428 mL |
| DMSO | 5 mM | 0.3307 mL | 1.6537 mL | 3.3074 mL | 8.2686 mL |
| 10 mM | 0.1654 mL | 0.8269 mL | 1.6537 mL | 4.1343 mL | |
| 15 mM | 0.1102 mL | 0.5512 mL | 1.1025 mL | 2.7562 mL | |
| 20 mM | 0.0827 mL | 0.4134 mL | 0.8269 mL | 2.0671 mL | |
| 25 mM | 0.0661 mL | 0.3307 mL | 0.6615 mL | 1.6537 mL | |
| 30 mM | 0.0551 mL | 0.2756 mL | 0.5512 mL | 1.3781 mL | |
| 40 mM | 0.0413 mL | 0.2067 mL | 0.4134 mL | 1.0336 mL | |
| 50 mM | 0.0331 mL | 0.1654 mL | 0.3307 mL | 0.8269 mL | |
| 60 mM | 0.0276 mL | 0.1378 mL | 0.2756 mL | 0.6890 mL | |
| 80 mM | 0.0207 mL | 0.1034 mL | 0.2067 mL | 0.5168 mL | |
| 100 mM | 0.0165 mL | 0.0827 mL | 0.1654 mL | 0.4134 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ceftaroline Related Classifications
HY-105049 Related Classifications
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Keywords
- Ceftaroline
- 189345-04-8
- T-91825
- PPI-0903M
- T91825
- T 91825
- Bacterial
- Antibiotic
- gram-negative bacteria
- MRSA
- gram-positive bacteria
- Enterococcus faecalis
- community-acquired pneumonia
- penicillin-binding proteins 2A
- penicillin-binding proteins 2
- complicated skin and soft tissue infections
- bacterial peptidoglycan
- anaerobic bacteria
- Inhibitor
- inhibitor
- inhibit