Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
25mg |
|
||
50mg |
|
||
100mg |
|
||
250mg |
|
||
500mg |
|
||
Other Sizes |
|
Purity: ≥98%
Cadazolid, also known ACT-179811, is a novel fluoroquinolone-oxazolidinone antibiotic and a protein synthesis inhibitor. Cadazolid may be potentially useful for the treatment of Clostridium difficile infection. Cadazolid exhibits potent in vitro activity against Clostridium difficile, including the epidemic BI/NAP1/027 strain. Clostridium difficile infection (CDI), the main cause of nosocomial infectious diarrhea, results from the growth of toxin-producing C. difficile in the colon following disruption of the normal enteric microbiota, usually as a consequence of antibiotic therapy.
Targets |
Oxazolidinone
|
---|---|
ln Vitro |
A novel antibiotic called cadezolide is being developed to treat diarrhea caused by Clostridium difficile[1]. All strains of Clostridium difficile, including those resistant to moxifloxacin and linezolid, are susceptible to the effects of cadazolid (MIC90 0.125, range 0.03-0.25 mg/L). In comparison to moxifloxacin, linezolid, metronidazole, and vancomycin, the cadazolid geometric mean MIC is 152-fold, 16-fold, 9-fold, and 7-fold lower, respectively. With no sign of recurrence, both cadazolid dosing regimens quickly lower cytotoxin and Clostridium difficile viable counts. Cadazolid levels last for 14 days after dosage, remaining 50–100 times supra-MIC. With the exception of bifidobacteria, cadezolides only slightly inhibit the counts of Lactobacillus spp. and members of the Bacteroides fragilis group of the enumerated gut microflora. There is no proof that strains resistant to linezolid, quinolones, or cadazolid have been chosen[2].
|
ln Vivo |
If taken twice daily for ten days, cadmiolid up to 3000 mg is well tolerated. There is no correlation found between adverse events and treatment duration or dosage; headaches are the most frequent adverse event. Cadazolid plasma concentrations are minimal. No plasma concentrations greater than 3.3 ng/mL or greater than 6.9 ng/mL following ten days of consecutive doses are seen. After a single 300 mg dose, food increased the mean Cmax from 0.73 to 1.87 ng/mL and the mean AUC0–t from 3.13 to 15.69 ng·h/mL. Less than dose-proportional increases in systemic exposure to cadazolid occur across doses. 81.0%–93.5% is the average cumulative faecal recovery. Less than 0.015% of unchanged compound is recovered in the urine[1].
|
References |
|
Molecular Formula |
C29H29F2N3O8
|
---|---|
Molecular Weight |
585.56
|
Exact Mass |
585.1923
|
Elemental Analysis |
C, 59.48; H, 4.99; F, 6.49; N, 7.18; O, 21.86
|
CAS # |
1025097-10-2
|
Related CAS # |
1025097-10-2
|
Appearance |
Solid powder
|
SMILES |
O=C(C1=CN(C2CC2)C3=C(C=C(F)C(N4CCC(O)(COC5=CC=C(N6C(O[C@@H](CO)C6)=O)C=C5F)CC4)=C3)C1=O)O
|
InChi Key |
XWFCFMXQTBGXQW-GOSISDBHSA-N
|
InChi Code |
InChI=1S/C29H29F2N3O8/c30-21-10-19-23(33(16-1-2-16)13-20(26(19)36)27(37)38)11-24(21)32-7-5-29(40,6-8-32)15-41-25-4-3-17(9-22(25)31)34-12-18(14-35)42-28(34)39/h3-4,9-11,13,16,18,35,40H,1-2,5-8,12,14-15H2,(H,37,38)/t18-/m1/s1
|
Chemical Name |
1-Cyclopropyl-6-fluoro-7-[4-({2-fluoro-4-[(5R)-5-(hydroxymethyl)-2-oxo-1,3-oxazolidin-3-yl]phenoxy}methyl)-4-hydroxypiperidin-1-yl]-4-oxo-1,4-dihydroquinolin-3-carboxylic acid
|
Synonyms |
ACT-179811; ACT 179811; ACT179811; Cadazolid.
|
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 (~170.78 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.27 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.27 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 3: 10% DMSO+90% (20% SBE-β-CD in Saline): ≥ 2.5 mg/mL (4.27 mM)  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7078 mL | 8.5388 mL | 17.0777 mL | |
5 mM | 0.3416 mL | 1.7078 mL | 3.4155 mL | |
10 mM | 0.1708 mL | 0.8539 mL | 1.7078 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.