Antibacterial Solithromycin binds to the large 50S subunit of the ribosome and inhibits protein biosynthesis. The mean 50% inhibitory concentrations (IC50s) for Solithromycin inhibition of cell viability, protein synthesis, and growth rate were 7.5, 40, and 125 ng/ml for Streptococcus pneumoniae,Staphylococcus aureus, and Haemophilus influenzae, respectively.
| Cell Experiment | |
|---|---|
| Cell lines | S. aureus cells |
| Preparation method | For S. pneumoniae, 12 9-ml cultures of cells comprised of one control set and one set with solithromycin at 7.5 ng/ml were grown to a Klett reading of 15. |
| Concentrations | 7.5 ng/ml |
| Incubation time | 15-min |
| Animal Experiment | |
|---|---|
| Animal models | donor mic |
| Formulation | DMSO |
| Dosages | 100 mg/kg |
| Administration | i.v. |
| Molecular Weight | 845.01 |
| Formula | C43H65FN5O10 |
| CAS Number | 760981-83-7 |
| Form | Solid |
| Solubility (25°C) | 32 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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