Potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 430.41. Batch specific molecular weights may vary from batch to batch due to solvent 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 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
If you know of a relevant reference for AMG 517, please let us know.
View Related Products by Product Action
Keywords: AMG 517, AMG 517 supplier, AMG517, potent, TRPV1, transient, potential, channels, antagonists, pain, antihyperalgesia, TRPV, 5995, Tocris Bioscience
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.)
Have you used AMG 517?
Submit a review and receive an Amazon gift card.
$10US/$10CAN/€7/£6 gift card for a review without an image
$25US/$25CAN/€18/£15 gift card for a review with an image
*Offer only valid in the USA / Canada, UK and EuropeSubmit a Review
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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.