product name Fidaxomicin
Description: Fidaxomicin (also called OPT-80, PAR-101) is a narrow spectrum antibiotic that inhibits RNA polymerase sigma subunit. 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.
References: Clin Infect Dis. 2012 Feb 15;54(4):568-74.
1058.04
Formula
C52H74Cl2O18
CAS No.
873857-62-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (94.5 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
OPT-80, PAR-101
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19413345
| In Vitro |
In vitro activity: 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Clin Infect Dis. 2012 Feb 15;54(4):568-74. |
