Size | Price | Stock | Qty |
---|---|---|---|
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
1g |
|
||
2g |
|
||
Other Sizes |
|
Purity: ≥98%
Cefditoren Pivoxil (also named ME-1207) is a broad-spectrum and 3rd-generation antibiotic against Gram-negative and Gram-positive bacteria. Cefditoren has MIC50/MIC90 results for Moraxella catarrhalis and Haemophilus influenzae of 0.12/0.5 and < or = 0.008/0.015 mg/mL, respectively. Cefditoren (MIC(90), 0.5 mg/mL) is 4- to 128-fold more active than comparison beta-lactams against the pneumoococci and was the most potent beta-lactam (including penicillin) versus beta-haemolytic streptococci. Cefditoren (MIC(90) in mg/mL/% susceptible) activity against all tested H. influenzae (0.03/100) and M. catarrhalis (0.06-0.5/100) is comparable to Cefixime and significantly greater than cefaclor.
Targets |
β-lactam
|
||
---|---|---|---|
ln Vitro |
Cefditoren has MIC50/MIC90 results for Moraxella catarrhalis and Haemophilus influenzae of 0.12/0.5 and < or = 0.008/0.015 mg/mL, respectively. Cefditoren (MIC(90), 0.5 mg/mL) is 4- to 128-fold more active than comparison beta-lactams against the pneumoococci and was the most potent beta-lactam (including penicillin) versus beta-haemolytic streptococci. Cefditoren (MIC(90) in mg/mL/% susceptible) activity against all tested H. influenzae (0.03/100) and M. catarrhalis (0.06-0.5/100) is comparable to Cefixime and significantly greater than cefaclor. Cefditoren pharmacokinetics demonstrate a T(1/2) of 1.5-2 hours and C(max) values of 2.8 and 4.6 mg/mL, respectively with 200 or 400 mg doses of Cefditoren pivoxil. Cefditoren possesses a broad-spectrum of cidal antibacterial activity against both Gram-positive and Gram-negative species with stability to many beta-lactamases of clinical importance. Cefditoren is also effective against methicillin-susceptible strains of Staphylococcus aureus. Cefditoren has compared favorably against other orally administered antibiotics used against the most commonly isolated respiratory tract pathogens. Cefditoren up-regulates the expression levels of Mrp2, Bcrp and Oat2, and down-regulate P-gp and Oct1 mRNA expression.
|
||
ln Vivo |
|
||
Animal Protocol |
|
||
References |
Diagn Microbiol Infect Dis.1998 Aug;31(4):573-8;Diagn Microbiol Infect Dis.2000 Jun;37(2):99-105;Drugs Exp Clin Res.1994;20(4):127-47.
|
Molecular Formula |
C25H28N6O7S3
|
|
---|---|---|
Molecular Weight |
620.72
|
|
Exact Mass |
620.12
|
|
Elemental Analysis |
C, 48.38; H, 4.55; N, 13.54; O, 18.04; S, 15.50
|
|
CAS # |
117467-28-4
|
|
Related CAS # |
Cefditoren sodium;104146-53-4;Cefditoren-13C,d3
|
|
Appearance |
Solid powder
|
|
SMILES |
CC1=C(SC=N1)/C=C\C2=C(N3[C@@H]([C@@H](C3=O)NC(=O)/C(=N\OC)/C4=CSC(=N4)N)SC2)C(=O)OCOC(=O)C(C)(C)C
|
|
InChi Key |
AFZFFLVORLEPPO-UVYJNCLZSA-N
|
|
InChi Code |
InChI=1S/C25H28N6O7S3/c1-12-15(41-10-27-12)7-6-13-8-39-21-17(29-19(32)16(30-36-5)14-9-40-24(26)28-14)20(33)31(21)18(13)22(34)37-11-38-23(35)25(2,3)4/h6-7,9-10,17,21H,8,11H2,1-5H3,(H2,26,28)(H,29,32)/b7-6-,30-16-/t17-,21-/m1/s1
|
|
Chemical Name |
(pivaloyloxy)methyl(6R,7R)-7-((Z)-2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido)-3-((Z)-2-(4-methylthiazol-5-yl)vinyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate
|
|
Synonyms |
|
|
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 |
|
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~100 mg/mL ( ~161.1 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. View More
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. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (4.03 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6110 mL | 8.0552 mL | 16.1103 mL | |
5 mM | 0.3222 mL | 1.6110 mL | 3.2221 mL | |
10 mM | 0.1611 mL | 0.8055 mL | 1.6110 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.