Ceftaroline fosamil [400827-46-5]

Cat# HY-14737-5mg

Size : 5mg

Brand : MedChemExpress

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Phone : +1 850 650 7790

Description

Ceftaroline fosamil (TAK-599), a cephalosporin derivative, is an N-phosphono proagent of anti-methicillin-resistant Staphylococcus aureus (MRSA) T-91825. Ceftaroline fosamil can be used for the research of MRSA infection[1][2][3].

IC50 & Target

β-lactam

 

In Vivo

Ceftaroline fosamil (s.c.) shows protective effects against experimental systemic infection caused by S. aureus N133 in mice, with ED50s of 1.60-2.37 mg/kg[1].
Ceftaroline fosamil (10 mg/kg; s.c.) disappeares rapidly and converts smoothly into T-91825 in blood of rats and monkeys[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

744.74

Formula

C24H25N8O10PS4

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C1[C@@H](NC(/C(C2=NSC(NP(O)(O)=O)=N2)=N\OCC)=O)[C@@]3(23)SCC(SC4=NC(C5=CC=[N+](C)C=C5)=CS4)=C(C(O)=O)N13.CC([O-])=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (55.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3428 mL 6.7138 mL 13.4275 mL
5 mM 0.2686 mL 1.3428 mL 2.6855 mL
View the 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; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (2.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (2.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

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