Fosnetupitant chloride monohydrochloride, the active molecule of the methylene phosphate precursor of Netupitant, is also an NK1 antagonist with pKi values of 9.5 and 6.1 for human NK1 and NK3 receptors, respectively.
Molecular Weight | 761.52 |
Formula | C31H37Cl2F6N4O5P |
CAS Number | 1643757-72-5 |
Form | Solid |
Storage | 4°C, dry, sealed |
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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