| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Oxazolidinone
Cadazolid targets bacterial protein synthesis. While the exact mode of action has yet to be fully elucidated, it is known to inhibit bacterial protein synthesis, leading to bacterial cell death. It is a potent inhibitor of protein synthesis in C. difficile and also inhibits the production of toxins and the formation of spores, which are critical for the pathogenesis and transmission of the infection. |
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| 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].
In vitro, Cadazolid demonstrates potent activity against C. difficile. It is active against all strains of C. difficile, including those resistant to moxifloxacin and linezolid. It has a MIC90 of 0.125 mg/L (range 0.03-0.25 mg/L) against clinical isolates. It also shows a low propensity for resistance formation. Its activity is superior to that of moxifloxacin. |
| 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].
In vivo, Cadazolid has shown efficacy in preclinical models of C. difficile infection (CDI). In the human gut CDAD model, it demonstrated potent activity. Its ability to inhibit toxin production and spore formation in addition to bacterial growth makes it a promising agent for treating CDI and reducing the risk of recurrence. |
| Enzyme Assay |
The in vitro activity of Cadazolid against C. difficile is determined using standard antimicrobial susceptibility testing methods. In a typical protocol, the minimum inhibitory concentration (MIC) is determined by broth microdilution or agar dilution methods according to CLSI guidelines. The MIC90, the concentration required to inhibit the growth of 90% of isolates, is calculated.
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| Cell Assay |
Cellular assays for Cadazolid involve studying its effects on C. difficile growth and toxin production. In a typical protocol, C. difficile is cultured in broth, and the effect of Cadazolid on bacterial growth is measured by optical density. The production of toxins A and B is measured by ELISA. Spore formation is assessed by plating and counting colonies after heat treatment.
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| Animal Protocol |
The in vivo efficacy of Cadazolid has been evaluated in animal models of C. difficile infection, such as the hamster model of CDI. In these studies, animals are infected with C. difficile and then treated with Cadazolid. The primary endpoints are survival and the reduction of C. difficile counts and toxin levels in the feces. These studies confirm its in vivo efficacy and support its clinical development.
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| ADME/Pharmacokinetics |
Cadazolid is an oxazolidinone antibiotic. It has a molecular weight of 550.56 and a molecular formula of C₂₉H₃₁FN₆O₆. It is being developed as an oral treatment for C. difficile infection. Its pharmacokinetic properties, including its high concentration in the gastrointestinal tract, are favorable for treating CDI.
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| Toxicity/Toxicokinetics |
Cadazolid is a new antibiotic being developed for the treatment of C. difficile infection. Its toxicity profile is being evaluated in preclinical and clinical studies. As an inhibitor of bacterial protein synthesis, it is expected to have a favorable safety profile with minimal systemic absorption. Its activity is primarily localized to the gastrointestinal tract, where it exerts its antibacterial effects.
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| References |
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| Additional Infomation |
Carzolid has been used in research trials for the treatment of Clostridium difficile infections. Carzolid is an oxazolidinone antibiotic active against Gram-positive bacteria, including Clostridium difficile. Although the exact mechanism of action of carzolid is not fully understood, after administration, it inhibits bacterial protein synthesis and leads to bacterial cell death.
Drug Indications Treatment of Clostridium difficile infections Cadazolid (ACT-179811) is a novel oxazolidinone antibiotic with potent activity against Clostridium difficile. It inhibits bacterial protein synthesis and strongly inhibits toxin production and spore formation. It is active against strains resistant to moxifloxacin and linezolid and has a low propensity for resistance formation. It is being developed as a treatment for C. difficile-associated diarrhea (CDAD). |
| Molecular Formula |
C29H29F2N3O8
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|---|---|
| Molecular Weight |
585.56
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| Exact Mass |
585.192
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| Elemental Analysis |
C, 59.48; H, 4.99; F, 6.49; N, 7.18; O, 21.86
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| CAS # |
1025097-10-2
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| Related CAS # |
1025097-10-2
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| PubChem CID |
44242317
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| Appearance |
White to light yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
832.6±65.0 °C at 760 mmHg
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| Flash Point |
457.4±34.3 °C
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| Vapour Pressure |
0.0±3.2 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
1.73
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
42
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| Complexity |
1100
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC1C=C2C(C(C(=O)O)=CN(C2=CC=1N1CCC(COC2C=CC(=CC=2F)N2C(=O)O[C@@H](CO)C2)(CC1)O)C1CC1)=O
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| InChi Key |
XWFCFMXQTBGXQW-GOSISDBHSA-N
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| 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
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| 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
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| Synonyms |
ACT-179811; ACT 179811; ACT179811; Cadazolid.
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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 |
| 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 : ~100 mg/mL (~170.78 mM)
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|---|---|
| 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.
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