AMG 517

Pricing Availability Delivery Time Qty
Cat.No. 5995 - AMG 517 | C20H13F3N4O2S | CAS No. 659730-32-2
Description: Potent TRPV1 antagonist
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.

Technical Data

M. Wt 430.41
Formula C20H13F3N4O2S
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 659730-32-2
PubChem ID 16007367
InChI Key YUTIXVXZQIQWGY-UHFFFAOYSA-N
Smiles O=C(NC(S1)=NC(C1=CC=C2)=C2OC3=NC=NC(C4=CC=C(C(F)(F)F)C=C4)=C3)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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 43.04 100

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.

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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 Target

View Related Products by Product Action

View all TRPV Antagonists

Keywords: AMG517 potent TRPV1 transient potential channels antagonists pain antihyperalgesia TRPV

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? If so please let us know.

Commented out for usability testing

Reviews

TODO: Add Reviews

Literature in this Area

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

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.

Pathways for AMG 517

Protocols

TODO: Add Protocols