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Cefoselis Sulfate (FK-037)

Alias: Cefoselis sulfate; Cefoselis (sulfate); FK 037; 6EY42207VS; Cefoselis sulfate (JAN);
Cat No.:V2035 Purity: ≥98%
Cefoselis (also known as FK 037 Sulfate)is a widely used beta-lactam antibiotic of the cephalosporin class.
Cefoselis Sulfate (FK-037)
Cefoselis Sulfate (FK-037) Chemical Structure CAS No.: 122841-12-7
Product category: Bacterial
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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Other Forms of Cefoselis Sulfate (FK-037):

  • Cefoselis
  • Cefoselis hydrochloride
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Cefoselis (also known as FK 037 Sulfate) is a widely used beta-lactam antibiotic of the cephalosporin class. Cefoselis inhibits GABA-induced currents in a concentration-dependent manner with IC50 of 185 mM. Cefoselis possesses a superior antistaphylococcal activity on MSSA isolates to both other compounds being however equal active to Cefepime and Cefpirome on multiresistant enterobacteriaceae. Cefoselis is dose-dependently appeared in brain extracellular fluid in proportion to its blood level. Cefoselis, a new parenteral cephalosporin, is active against clinical isolates of both gram-positive and gram-negative aerobic bacteria.

Biological Activity I Assay Protocols (From Reference)
Targets
β-lactam
ln Vitro
Cefoselis inhibits GABA-induced currents in a concentration-dependent manner with IC50 of 185 mM. Cefoselis possesses a superior antistaphylococcal activity on MSSA isolates to both other compounds being however equal active to Cefepime and Cefpirome on multiresistant enterobacteriaceae. Cefoselis is dose-dependently appeared in brain extracellular fluid in proportion to its blood level. Cefoselis, a new parenteral cephalosporin, is active against clinical isolates of both gram-positive and gram-negative aerobic bacteria.
ln Vivo
Cefoselis elicits a massive elevation of extracellular glutamate concentration in normal rats. Cefoselis (50 mg/animal)-induced convulsions are prevented by pretreatment with 5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801), diazepam and phenobarbital (ED(50) values (mg/kg) of 0.78, 1.59 and 33.0, respectively), but not by carbamazepine or phenytoin.
Animal Protocol
50 mg/animal
Rats
References

[1]. Cefoselis, a beta-lactam antibiotic, easily penetrates the blood-brain barrier and causes seizure independently by glutamate release. J Neural Transm (Vienna). 2004 Dec;111(12):1523-35.

[2]. In vitro activities of cefoselis compared to β-lactams and other antibacterial agents aganst gram-positive and gram-negative clinical isolates. Chinese Journal of Infection and Chemotherapy, 2011. 4: p. 002.

[3]. King, A., L. Bethune, and I. Phillips, The Comparative In Vitro Activity of FK-037 (Cefoselis), a New Broad-Spectrum Cephalosporin. Clin Microbiol Infect, 1995. 1(1): p. 13-17.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H24N8O10S3
Molecular Weight
620.64
Elemental Analysis
C, 36.77; H, 3.90; N, 18.05; O, 25.78; S, 15.50
CAS #
122841-12-7
Related CAS #
Cefoselis;122841-10-5;Cefoselis hydrochloride;911212-25-4
Appearance
Solid powder
SMILES
CO/N=C(/C1=CSC(=N1)N)\C(=O)N[C@H]2[C@@H]3N(C2=O)C(=C(CS3)CN4C=CC(=N)N4CCO)C(=O)O.OS(=O)(=O)O
InChi Key
LZOLCSVRFKCSEM-ZQCAECPKSA-N
InChi Code
InChI=1S/C19H22N8O6S2.H2O4S/c1-33-24-12(10-8-35-19(21)22-10)15(29)23-13-16(30)27-14(18(31)32)9(7-34-17(13)27)6-25-3-2-11(20)26(25)4-5-28;1-5(2,3)4/h2-3,8,13,17,20,28H,4-7H2,1H3,(H2,21,22)(H,23,29)(H,31,32);(H2,1,2,3,4)/b20-11?,24-12-;/t13-,17-;/m1./s1
Chemical Name
(6R,7R)-7-((Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido)-3-((2-(2-hydroxyethyl)-3-imino-2,3-dihydro-1H-pyrazol-1-yl)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid compound with sulfuric acid (1:1)
Synonyms
Cefoselis sulfate; Cefoselis (sulfate); FK 037; 6EY42207VS; Cefoselis sulfate (JAN);
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage.  (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
Solubility Data
Solubility (In Vitro)
Water : 5~14.29 mg/mL(~23.02 mM)
DMSO : 3~100 mg/mL ( 4.83~161.12 mM )
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.03 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 25.0 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: ≥ 2.5 mg/mL (4.03 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 25.0 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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (4.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.03 mM)

Solubility in Formulation 5: 25 mg/mL (40.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.6112 mL 8.0562 mL 16.1124 mL
5 mM 0.3222 mL 1.6112 mL 3.2225 mL
10 mM 0.1611 mL 0.8056 mL 1.6112 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

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