All AbMole products are for research use only, cannot be used for human consumption.
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 |
| Related TRP Channel Products |
|---|
| SB-705498
SB-705498 is a potent, selective and orally bioavailable transient receptor potential vanilloid 1 (TRPV1) receptor antagonist with a pIC50 of 7.1. |
| HC-030031
HC-030031 is a selective TRPA1 blocker, antagonizing TRPA1-mediated calcium influx induced by AITC and formalin (IC50 = 6.2 and 5.3 μM, respectively). |
| Icilin
Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel. |
| Phenazopyridine hydrochloride
Phenazopyridine HCl is a competitive SARM1 inhibitor as well as a TRPM8 antagonist with an IC50 for SARM1 inhibition of 145 μM. It has local anesthetic/analgesic activity and can be used in studies related to traumatic brain injury, peripheral neuropathy, and neurodegenerative diseases. |
| Probenecid
Probenecid is a classical competitive inhibitor of organic anion transport, which is also a TRPV2 agonist and an inhibitor of TAS2R16. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
