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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Ceftaroline fosamil (formerly also known as TAK-599 and PPI-0903) is a new generation of antibiotic belonging to the cephalosporin class with activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Ceftaroline fosamil retains the activity of later-generation cephalosporins having broad-spectrum activity against Gram-negative bacteria. It is currently being investigated for community-acquired pneumonia and complicated skin and skin structure infection.
Targets |
β-lactam
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ln Vivo |
With ED50s of 1.60–2.37 mg/kg, ceftaroline fosamil (s.c.) protects mice from experimental systemic infection caused by S. aureus N133[1].
In the blood of rats and monkeys, ceftaroline fosamil (10 mg/kg; s.c.) vanishes quickly and smoothly transforms into T-91825[1]. |
Animal Protocol |
Using the neutropenic lung infection model, 17 clinical S. aureus isolates (2 MSSA, 15 MRSA) are investigated. For a duration of 24 hours, groups of six mice are treated with Ceftaroline fosamil starting three hours after inoculation. Doses of ceftaroline fosamil are injected subcutaneously in increments of 0.2 mL. Normal saline is given to control animals in the same amounts, ways, and intervals as the treatment plans[1].
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References |
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Molecular Formula |
C22H21N8O8PS4
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Molecular Weight |
744.7
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Exact Mass |
684.01
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Elemental Analysis |
C, 38.71; H, 3.38; N, 15.05; O, 21.48; P, 4.16; S, 17.22
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CAS # |
400827-46-5
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Related CAS # |
Ceftaroline fosamil (hydrate)(acetate);400827-55-6;Ceftaroline fosamil (inner);229016-73-3
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Appearance |
Solid powder
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SMILES |
O=C(O)C(N1[C@@]([H])([C@@H](C1=O)NC(/C(C2=NSC(NP(O)(O)=O)=N2)=N\OCC)=O)SC3)=C3SC4=NC(C5=CC=[N+]
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InChi Key |
UGHHNQFYEVOFIV-VRDMTWHKSA-N
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InChi Code |
InChI=1S/C22H21N8O8PS4.C2H4O2/c1-3-38-26-13(16-25-21(43-28-16)27-39(35,36)37)17(31)24-14-18(32)30-15(20(33)34)12(9-40-19(14)30)42-22-23-11(8-41-22)10-4-6-29(2)7-5-10;1-2(3)4/h4-8,14,19H,3,9H2,1-2H3,(H4-,24,25,27,28,31,33,34,35,36,37);1H3,(H,3,4)/b26-13-;/t14-,19-;/m1./s1
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Chemical Name |
4-(2-(((6R,7R)-2-carboxy-7-((Z)-2-(ethoxyimino)-2-(5-(phosphonoamino)-1,2,4-thiadiazol-3-yl)acetamido)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl)thio)thiazol-4-yl)-1-methylpyridin-1-ium acetate
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Synonyms |
T-91825; T 91825; T91825; Teflaro; Zinforo;TAK 599; TAK599; TAK-599; PPI 0903; PP 0903; PPI-0903;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 73~100 mg/mL ( 98.02~134.28 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (2.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (2.79 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3428 mL | 6.7141 mL | 13.4282 mL | |
5 mM | 0.2686 mL | 1.3428 mL | 2.6856 mL | |
10 mM | 0.1343 mL | 0.6714 mL | 1.3428 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.