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Cadazolid

Cat. No. M6091
Cadazolid Structure
Synonym:

ACT-179811

Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 139  USD139 In stock
50mg USD 415  USD415 In stock
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Quality Control & Documentation
Biological Activity

Cadazolid is a new antibiotic in development for the treatment of Clostridium difficile-associated diarrhea. Cadazolid is active against all (including linezolid- and moxifloxacin-resistant) Clostridium difficile strains (MIC90 0.125, range 0.03-0.25 mg/L). The cadazolid geometric mean MIC is 152-fold, 16-fold, 9-fold and 7-fold lower than those of moxifloxacin, linezolid, metronidazole and vancomycin, respectively. Both cadazolid dosing regimens rapidly reduce Clostridium difficile viable counts and cytotoxin with no evidence of recurrence.

Protocol (for reference only)
Cell Experiment
Cell lines C. difficile
Preparation method Experiments to assess the effects of cadazolid and comparator antibiotics on C. difficile toxin formation were done by determination of toxin A and B concentrations in stationary-phase cultures of toxigenic C. difficile
Concentrations 0.3% (vol/vol) DMSO
Incubation time 24 h
Animal Experiment
Animal models Hamster model of CDAD
Formulation 0.5% [wt/wt] methylcellulose containing 0.05% [wt/vol] Tween 80
Dosages 10 mg/kg
Administration gavage
Chemical Information
Molecular Weight 505.55
Formula C29H29F2N3O8
CAS Number 1025097-10-2
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Louie T, et al. Antimicrob Agents Chemother. Multicenter, Double-Blind, Randomized, Phase 2 Study Evaluating the Novel Antibiotic Cadazolid in Patients with Clostridium difficile Infection.

[2] Locher HH, et al. Antimicrob Agents Chemother. In vitro and in vivo antibacterial evaluation of cadazolid, a new antibiotic for treatment of Clostridium difficile infections.

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