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Ceftaroline fosamil

Katalog-Nr.GC35646

Ceftarolinfosamil (TAK-599), ein Cephalosporin-Derivat, ist ein N-Phosphono-Prodrug des anti-Methicillin-resistenten Staphylococcus aureus (MRSA) T-91825.

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Ceftaroline fosamil Chemische Struktur

Cas No.: 400827-46-5

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10mM (in 1mL DMSO)
157,00 $
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5mg
96,00 $
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10mg
152,00 $
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50mg
558,00 $
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Sample solution is provided at 25 µL, 10mM.

Description of Ceftaroline fosamil

Ceftaroline fosamil is a cephalosporin with activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA).

Ceftaroline fosamil is effective against all 10 MRSA isolates used in the dose-ranging studies and requires approximately 17 to 43% fT>MIC (the percentage of time that free drug concentrations remain above the MIC) to produce a 1-log10 kill[1]. The Ceftaroline Fosamil treatment results in mean reductions of 1.1 to 2.4 log10 CFU, with no relationship to the Ceftaroline Fosamil MIC. The use of high inocula does not affect the Ceftaroline Fosamil efficacy against the three strains tested, with mean decreases of 2.0 to 3.0 log10 CFU[2].

[1]. Bhalodi AA, et al. Efficacy of ceftaroline fosamil in a staphylococcal murine pneumonia model. Antimicrob Agents Chemother. 2012 Dec;56(12):6160-5. [2]. So W, et al. Comparison of in vivo and in vitro pharmacodynamics of a humanized regimen of 600 milligrams of Ceftaroline Fosamil every 12 hours against Staphylococcus aureus at initial inocula of 106 and 108 CFU per milliliter. Antimicrob Agents Chemother. 2014 Nov;58(11):6931-3.

Protocol of Ceftaroline fosamil

Animal experiment:

Seventeen clinical S. aureus isolates (2 MSSA, 15 MRSA) are studied using the neutropenic lung infection model. Beginning 3 h after inoculation, groups of six mice receive treatment with Ceftaroline fosamil over a 24 h period. Ceftaroline fosamil doses are administered as 0.2 mL subcutaneous injections. Control animals are administered normal saline at the same volume, route, and frequency as the treatment regimens[1].

References:

[1]. Bhalodi AA, et al. Efficacy of ceftaroline fosamil in a staphylococcal murine pneumonia model. Antimicrob Agents Chemother. 2012 Dec;56(12):6160-5.
[2]. So W, et al. Comparison of in vivo and in vitro pharmacodynamics of a humanized regimen of 600 milligrams of Ceftaroline Fosamil every 12 hours against Staphylococcus aureus at initial inocula of 106 and 108 CFU per milliliter. Antimicrob Agents Chemother. 2014 Nov;58(11):6931-3.

Chemical Properties of Ceftaroline fosamil

Cas No. 400827-46-5 SDF
Canonical SMILES O=C1[C@@H](NC(/C(C2=NSC(NP(O)(O)=O)=N2)=N\OCC)=O)[C@@]3([H])SCC(SC4=NC(C5=CC=[N+](C)C=C5)=CS4)=C(C(O)=O)N13.CC([O-])=O
Formula C24H25N8O10PS4 M.Wt 744.74
Löslichkeit DMSO: 30 mg/mL (40.28 mM and warming) Storage Store at 2-8°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Ceftaroline fosamil

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.3428 mL 6.7138 mL 13.4275 mL
5 mM 268.6 μL 1.3428 mL 2.6855 mL
10 mM 134.3 μL 671.4 μL 1.3428 mL
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In vivo Formulation Calculator (Clear solution) of Ceftaroline fosamil

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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