AMG 517 is a potent and selective TRPV1 antagonist, antagonizes capsaicin, proton, and heat activation of TRPV1 with IC50 of 0.76 nM, 0.62 nM and 1.3 nM.
 |
Source | Bioanalysis (2014). Figure 2. AMG-517 |
| Method | PK analysis | |
| Cell Lines | Male CD-1 mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 48 h | |
| Results | AMG 517 plasma concentration–time profiles for both collection techniques were superimposable |
 |
Source | Bioanalysis (2014). Figure 1. AMG-517 |
| Method | PK analysis | |
| Cell Lines | Male CD-1 mice | |
| Concentrations | 1 mg/kg | |
| Incubation Time | 48 h | |
| Results | Following sample extraction and LC–MS/MS analysis to determine the AMG 517 concentrations, the concentration–time profiles from manual DBS and whole blood were nearly indistinguishable |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague-Dawley rats |
| Formulation | Ora-Plus-5% Tween 80 |
| Dosages | 0.003-3 mg/kg |
| Administration | p.o. |
| Molecular Weight | 430.4 |
| Formula | C20H13F3N4O2S |
| CAS Number | 659730-32-2 |
| Solubility (25°C) | DMSO 68 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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