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Ceftaroline fosamil [400827-46-5]

Imprimer

Référence HY-14737-5mg

Conditionnement : 5mg

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Téléphone : +1 850 650 7790

Marque : MedChemExpress

Contactez votre distributeur local :

Téléphone : +1 850 650 7790

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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Ceftaroline fosamil Chemical Structure

CAS No. : 400827-46-5

This product is a controlled substance and not for sale in your territory.

Based on 2 publication(s) in Google Scholar

Other Forms of Ceftaroline fosamil:

Ceftaroline fosamil hydrate Obtenir un devis
Ceftaroline fosamil (inner) Obtenir un devis

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Description

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.

Essai clinique

Masse moléculaire

744.74

Formule

C₂₄H₂₅N₈O₁₀PS₄

CAS No.

400827-46-5

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(20)SCC(SC4=NC(C5=CC=[N+](C)C=C5)=CS4)=C(C(O)=O)N13.CC([O-])=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

-20°C, sealed storage, away from moisture

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (134.28 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
10 mM	0.1343 mL	0.6714 mL	1.3428 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.

Calculateur de molarité
Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (2.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureté et documentation

Purity: 99.98%

Select Batch:

Fiche technique (280 KB) SDS (563 KB)

COA (257 KB) HNMR (316 KB) LCMS (112 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37. [Content Brief]

[2]. Jacqueline C, et, al. In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model. Antimicrob Agents Chemother. 2007 Sep;51(9):3397-400. [Content Brief]

[3]. Parish D, et, al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9. [Content Brief]

Administration animale ^[1]	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]. MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références	[1]. Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37. [Content Brief] [2]. Jacqueline C, et, al. In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model. Antimicrob Agents Chemother. 2007 Sep;51(9):3397-400. [Content Brief] [3]. Parish D, et, al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9. [Content Brief]

Administration animale
^[1]

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].

MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

Références

[1]. Ishikawa T, et, al. TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: synthesis, physicochemical and pharmacological properties. Bioorg Med Chem. 2003 May 29;11(11):2427-37. [Content Brief]

[2]. Jacqueline C, et, al. In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model. Antimicrob Agents Chemother. 2007 Sep;51(9):3397-400. [Content Brief]

[3]. Parish D, et, al. Ceftaroline fosamil, a cephalosporin derivative for the potential treatment of MRSA infection. Curr Opin Investig Drugs. 2008 Feb;9(2):201-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.3428 mL	6.7138 mL	13.4275 mL	33.5688 mL
	5 mM	0.2686 mL	1.3428 mL	2.6855 mL	6.7138 mL
	10 mM	0.1343 mL	0.6714 mL	1.3428 mL	3.3569 mL
	15 mM	0.0895 mL	0.4476 mL	0.8952 mL	2.2379 mL
	20 mM	0.0671 mL	0.3357 mL	0.6714 mL	1.6784 mL
	25 mM	0.0537 mL	0.2686 mL	0.5371 mL	1.3428 mL
	30 mM	0.0448 mL	0.2238 mL	0.4476 mL	1.1190 mL
	40 mM	0.0336 mL	0.1678 mL	0.3357 mL	0.8392 mL
	50 mM	0.0269 mL	0.1343 mL	0.2686 mL	0.6714 mL
	60 mM	0.0224 mL	0.1119 mL	0.2238 mL	0.5595 mL
	80 mM	0.0168 mL	0.0839 mL	0.1678 mL	0.4196 mL
	100 mM	0.0134 mL	0.0671 mL	0.1343 mL	0.3357 mL

Ceftaroline fosamil [400827-46-5]

Référence HY-14737-5mg

Contactez votre distributeur local :

Marque : MedChemExpress

Contactez votre distributeur local :

Other Forms of Ceftaroline fosamil:

Voir tous les produits spécifiques à Isoform Antibiotic:

Calculateur de molarité

Calculateur de dilution

Complete Stock Solution Preparation Table

Ceftaroline fosamil Related Classifications

Keywords:

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