Emetine dihydrochloride hydrate is an alkaloid that has been found in ipecac root and has diverse biological activities. Emetine inhibits NF-κB signaling induced by TNF-α or IL-1β (IC50s = 2 and 4.2 μM, respectively, in a cell-based β-lactamase reporter assay), increases caspase-3/7 activity in ME180 cells (EC50 = 1.1 μM), and is cytotoxic to HeLa cells. It reduces the infectious virus yield and viral RNA copy numbers in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC50s = 0.46 and 0.5 μM, respectively). Emetine (5 mg/kg) induces emesis in ferrets, an effect that can be prevented by the serotonin (5-HT) receptor subtype 5-HT3 antagonist ondansetron.
| Molecular Weight | 571.58 |
| Formula | C29H40N2O4.2HCl.H2O |
| CAS Number | 7083-71-8 |
| Solubility (25°C) | Water 60 mg/mL |
| 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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