Ceftaroline hydrochloride
Based on 1 publication(s) in Google Scholar
Ceftaroline hydrochloride is a cephalosporin compound and the active form of Ceftaroline fosamil (HY-14737). Ceftaroline hydrochloride exhibits activity against Gram-positive bacteria, Gram-negative bacteria, and some anaerobic bacteria. Ceftaroline hydrochloride 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 hydrochloride can be used in research related to complicated skin and soft tissue infections, community-acquired pneumonia, Enterococcus faecalis infective endocarditis, and bacterial infections.
For research use only. We do not sell to patients.
- Purity : 98.0%
- Formula: C22H21ClN8O5S4
- Molecular Weight:641.17
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Storage:
-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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ceftaroline hydrochloride
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Biological Activity
Description
In Vitro
Ceftaroline hydrochloride (T-91825 hydrochloride) 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 (6-24 h) hydrochloride 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 hydrochloride, 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 hydrochloride, 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.
Chemical Information
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Appearance Solid
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Molecular Weight 641.17
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Formula C22H21ClN8O5S4
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Color Light yellow 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.Cl
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Shipping
Shipping with dry ice.
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Storage
-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
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (155.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocols
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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.
Purity & Documentation
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Data Sheet (293 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[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 |
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| DMSO | 1 mM | 1.5596 mL | 7.7982 mL | 15.5965 mL | 38.9912 mL |
| 5 mM | 0.3119 mL | 1.5596 mL | 3.1193 mL | 7.7982 mL | |
| 10 mM | 0.1560 mL | 0.7798 mL | 1.5596 mL | 3.8991 mL | |
| 15 mM | 0.1040 mL | 0.5199 mL | 1.0398 mL | 2.5994 mL | |
| 20 mM | 0.0780 mL | 0.3899 mL | 0.7798 mL | 1.9496 mL | |
| 25 mM | 0.0624 mL | 0.3119 mL | 0.6239 mL | 1.5596 mL | |
| 30 mM | 0.0520 mL | 0.2599 mL | 0.5199 mL | 1.2997 mL | |
| 40 mM | 0.0390 mL | 0.1950 mL | 0.3899 mL | 0.9748 mL | |
| 50 mM | 0.0312 mL | 0.1560 mL | 0.3119 mL | 0.7798 mL | |
| 60 mM | 0.0260 mL | 0.1300 mL | 0.2599 mL | 0.6499 mL | |
| 80 mM | 0.0195 mL | 0.0975 mL | 0.1950 mL | 0.4874 mL | |
| 100 mM | 0.0156 mL | 0.0780 mL | 0.1560 mL | 0.3899 mL |
Ceftaroline hydrochloride Related Classifications
HY-105049A Related Classifications
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Keywords
- Ceftaroline
- Bacterial
- Antibiotic
- Penicillin-binding protein (PBP)
- 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