Molecular Formula | C52H74Cl2O18 |
Molar Mass | 1058.04 |
Density | 1.33 |
Melting Point | 161 °C |
Boling Point | 1046.4±65.0 °C(Predicted) |
Solubility | Chloroform (Slightly, Heated), DMSO (Slightly, Heated), Methanol (Slightly) |
Appearance | powder |
Color | White to Off-White |
pKa | 5.09±0.35(Predicted) |
Storage Condition | 2-8°C |
Physical and Chemical Properties | Fedamycin is the fermentation product of actinoplanans actinomycetes or orange cyst fungus, belonging to a new 18-membered macrolide compound. Molecular weight 1058.04, molecular formula C32H74C12O18, in vivo can produce still active metabolite OP-1118. |
In vitro study | Fidaxomicin inhibits RNA polymerase by binding to the DNA template-RNA polymerase (RNAP) complex prior to the formation of the open RNAP-DNA complex, I .e., the start of transcription. Therefore, it inhibits protein synthesis. Therefore, apoptosis in susceptible organisms, such as C. difficile, is triggered. |
In vivo study | The minimum inhibitory concentration of fidaxomicin anti-C. difficile is 0.9978 to 2 μg/mL for 90% of the organisms. Blood concentrations below the lower limit of quantitation after single or multiple doses indicate that the Fidaxomicin is not systemically absorbed. In contrast, fecal concentrations of fidaxomicin were much higher and concentration-dependent. Cmax = 2 hours; Tmax = 5.2 ng/mL; Acc = 14 ng • hr/mL. Cmax was 2 hours; Tmax was 5.2 ng/mL; Acc = 14 Ng-h/mL. Fidaxomicin can be hydrolyzed into smaller active metabolites (OP-1118) by gastric acid or intestinal microparticles. The cytochrome enzyme system is not involved in the metabolism of fidaxomicin. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.945 ml | 4.726 ml | 9.451 ml |
5 mM | 0.189 ml | 0.945 ml | 1.89 ml |
10 mM | 0.095 ml | 0.473 ml | 0.945 ml |
5 mM | 0.019 ml | 0.095 ml | 0.189 ml |