Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury.
説明 | Fidaxomicin (Tiacumicin B) is a semisynthetic macrolide antibiotic used to treat Clostridium difficile-associated diarrhea in adults. Fidaxomicin has minimal systemic absorption and has not been linked to serum enzyme elevations during therapy or to instances of clinically apparent, acute liver injury. |
In vitro | Fidaxomicin acts as a RNA polymerase inhibitor by binding to the DNA template–RNA polymerase (RNAP) complex prior to the formation of the open RNAP-DNA complex in which transcription is initiated. Therefore it will inhibit protein synthesis. As a result, apoptosis is triggered in susceptible organisms such as C. difficile. [1] |
In vivo | The minimum inhibitory concentration for 90% of organisms for fidaxomicin against C. difficile is 0.9978 to 2 μg/mL. Fidaxomicin is not systemically absorbed as shown by a plasma concentrations below the lower limit of quantification after single-dose or multiple-dose. In contrast, fecal concentrations of fidaxomicin are much higher and are concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; AUC = 14 ng?hr/mL. Fidaxomicin is hydrolyzed by gastric acid or intestinal microsomes into a less active metabolite (OP-1118). The cytochrome enzyme system are not involved in the metabolism of fidaxomicin. [1] |
別名 | Tiacumicin B, OPT-80, Clostomicin B1, PAR-101 |
分子量 | 1058.04 |
分子式 | C52H74Cl2O18 |
CAS No. | 873857-62-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (56.71 mM)
You can also refer to dose conversion for different animals. 詳細
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Fidaxomicin 873857-62-6 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Antibacterial Antibiotic DNA/RNA Synthesis CDAD Clostridium difficile PAR101 difimicin Inhibitor orally active OPT 80 Tiacumicin B PAR 101 CDI inhibit OPT-80 Bacterial RNA polymerase OPT80 Clostomicin B1 PAR-101 inhibitor