Cadazolid (Synonyms: ACT-179811) |
| Catalog No.GC19085 |
Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1025097-10-2
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile.
Cadazolid is a new antibiotic in development for the treatment of Clostridium difficile-associated diarrhea[1]. 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. Cadazolid levels persists at 50-100-fold supra-MIC for 14 days post-dosing. Cadazolid inhibition of enumerated gut microflora is limited, with the exception of bifidobacteria; Bacteroides fragilis group and Lactobacillus spp. counts are unaffected. There is no evidence for selection of strains resistant to cadazolid, quinolones or linezolid[2].
Cadazolid is well tolerated up to 3000 mg given twice daily for 10 days. The most common adverse event is headache, with no observed relationship between dose or treatment duration and adverse events. Plasma concentrations of cadazolid are low. No plasma concentrations >3.3 ng/mL are observed after single doses or >6.9 ng/mL after 10 days of multiple doses. Food increased the mean Cmax from 0.73 to 1.87 ng/mL and mean AUC0-t from 3.13 to 15.69 ng.h/mL after a single 300 mg dose. The increase in systemic exposure to cadazolid across doses is less than dose-proportional. The mean cumulative faecal recovery is 81.0%-93.5%. Urinary recovery of unchanged compound is less than 0.015%[1].
References:
[1]. Baldoni D, et al. Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral doses. J Antimicrob Chemother. 2014 Mar;69(3):706-14.
[2]. Chilton CH, et al. In vitro activity of cadazolid against clinically relevant Clostridium difficile isolates and in an in vitro gut model of C. difficile infection. J Antimicrob Chemother. 2014 Mar;69(3):697-705.
Cell experiment: | MICs of cadazolid, metronidazole, vancomycin, moxifloxacin and linezolid are determined using agar incorporation for 100 Clostridium difficile isolates, including 30 epidemic strains (ribotypes 027, 106 and 001) with reduced metronidazole susceptibility, 2 linezolid-resistant isolates and 2 moxifloxacin-resistant isolates. The efficacy of two cadazolid dosing regimens (250 versus 750 mg/L twice daily for 7 days) to treat simulated CDI is evaluated. Microflora populations, Clostridium difficile total viable counts and spores, cytotoxin titres, possible emergence of cadazolid, linezolid or quinolone resistance, and antimicrobial concentrations are monitored throughout[2]. |
References: [1]. Baldoni D, et al. Cadazolid, a novel antibiotic with potent activity against Clostridium difficile: safety, tolerability and pharmacokinetics in healthy subjects following single and multiple oral doses. J Antimicrob Chemother. 2014 Mar;69(3):706-14. | |
| Cas No. | 1025097-10-2 | SDF | |
| Synonyms | ACT-179811 | ||
| Canonical 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 | ||
| Formula | C29H29F2N3O8 | M.Wt | 585.55 |
| Solubility | DMSO : ≥ 150 mg/mL (256.17 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7078 mL | 8.539 mL | 17.078 mL |
| 5 mM | 0.3416 mL | 1.7078 mL | 3.4156 mL |
| 10 mM | 0.1708 mL | 0.8539 mL | 1.7078 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *