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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.
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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 |
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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 | |
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| 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 |
| Related TRP Channel Products |
|---|
| Moringin
Moringin is a potent and selective TRPA1 ion channel natural agonist with an EC50 of 3.14 μM. Moringin does not activate or activates very weakly the vanilloids somatosensory channels TRPV1, TRPV2, TRPV3 and TRPV4, and the melastatin cooling receptor TRPM8. |
| (S)-ABT-102
(S)-ABT-102 is a potent TRPV1 antagonist, with an IC50 of 123 nM. (S)-ABT-102 can block the activation of TRPV1 by capsaicin. |
| Oleoyl Serotonin
Oleoyl Serotonin is a TRPV1 antagonist with IC50 value of 2.57 μM for human TRPV1. |
| ABT-102
ABT-102 (CHEMBL398338) is a potent and highly selective transient receptor potential vanilloid 1 (TRPV1) receptor antagonist. |
| MK-2295
MK-2295 (TRPV1 antagonist 5) is a potent TRPV1 antagonist. MK-2295 can be used for the research of chronic pain. |
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