CAS NO: | 1025097-10-2 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Cadazolid (ACT-179811) is a newoxazolidinoneantibiotic with potent activity againstClostridium difficile. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Cadazolid is a new antibiotic in development for the treatment ofClostridium difficile-associated diarrhea[1]. Cadazolid is active against all (including linezolid- and moxifloxacin-resistant)Clostridium difficilestrains (MIC900.125, 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 reduceClostridium difficileviable 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 fragilisgroup andLactobacillus spp.counts are unaffected. There is no evidence for selection of strains resistant to cadazolid, quinolones or linezolid[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 585.55 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C29H29F2N3O8 | ||||||||||||||||
CAS 号 | 1025097-10-2 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(170.78 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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