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• 产品描述： Cadazolid (ACT-179811) is a new oxazolidinone antibiotic with potent activity against Clostridium difficile.

• 靶点： Oxazolidinone;Antibacterial; Antibiotic

• 体外研究：
  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. 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

• 体内研究：
  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%

• 参考文献：
  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.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.708 ml	8.539 ml	17.078 ml
  5 mM	0.342 ml	1.708 ml	3.416 ml
  10 mM	0.171 ml	0.854 ml	1.708 ml
  50 mM	0.034 ml	0.171 ml	0.342 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *