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Biological Activity for AMG 517
AMG 517 is a potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.
Compound Libraries for AMG 517
Technical Data for AMG 517
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AMG 517
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for AMG 517
The following data is based on the product molecular weight 430.41. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.32 mL||11.62 mL||23.23 mL|
|5 mM||0.46 mL||2.32 mL||4.65 mL|
|10 mM||0.23 mL||1.16 mL||2.32 mL|
|50 mM||0.05 mL||0.23 mL||0.46 mL|
References for AMG 517
References are publications that support the biological activity of the product.
Gavva et al (2007) Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J.Pharmacol.Exp.Ther. 323 128 PMID: 17652633
Wang et al (2007) Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J.Med.Chem. 50 3528 PMID: 17585751
Doherty et al (2007) Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J.Med.Chem. 50 3515 PMID: 17585750
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Citations for AMG 517
Citations are publications that use Tocris products.
Currently there are no citations for AMG 517. Do you know of a great paper that uses AMG 517 from Tocris? Please let us know.
Reviews for AMG 517
Average Rating: 5 (Based on 1 Review.)
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.