Home / Pharmacology / Ion Channels / Transient Receptor Potential Channels / TRPM / TRPM Antagonists / AMG 333

AMG 333

Cat. No. 6874 Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Cat.No. 6874 - AMG 333 | C20H12F5N3O4 | CAS No. 1416799-28-4
Description: Potent and selective TRPM8 antagonist; active in vivo
Chemical Name: 6-[[[(S)-(3-Fluoro-2-pyridinyl)[3-fluoro-4-(trifluoromethoxy)phenyl]methyl]amino]carbonyl]-3-pyridinecarboxylic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective TRPM8 antagonist (IC50 values are 13 and 20 nM for hTRPM8 and rTRPM8, respectively). Displays high selectivity over other TRP channels (IC50 >20 μM, TRPV1/V3/V4/A1). Inhibits icilin-induced wet-dog shake in rats and suppresses cold-induced increases in blood pressure in the rat cold-pressor test.

Technical Data

M. Wt 453.33
Formula C20H12F5N3O4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1416799-28-4
PubChem ID 71144018
InChI Key QEBYISWYMFIXOZ-INIZCTEOSA-N
Smiles OC(=O)C1=CC=C(N=C1)C(=O)N[C@@H](C1=CC(F)=C(OC(F)(F)F)C=C1)C1=C(F)C=CC=N1

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.33 100
ethanol 45.33 100

Preparing Stock Solutions

The following data is based on the product molecular weight 453.33. 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 2.21 mL 11.03 mL 22.06 mL
5 mM 0.44 mL 2.21 mL 4.41 mL
10 mM 0.22 mL 1.1 mL 2.21 mL
50 mM 0.04 mL 0.22 mL 0.44 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

References

References are publications that support the biological activity of the product.

Horne et al (2018) Discovery of TRPM8 antagonist (S)-6-(((3-Fluoro-4-(trifluoromethoxy)phenyl)(3-fluoropyridin-2-yl)methyl)carbamoyl)nicotinic acid (AMG 333), a clinical candidate for the treatment of migraine. J.Med.Chem. 61 8186 PMID: 30148953

If you know of a relevant reference for AMG 333, please let us know.

View Related Products by Target

View Related Products by Product Action

View all TRPM Antagonists

Keywords: AMG 333, AMG 333 supplier, AMG333, Potent, selective, TRPM8, antagonists, antagonism, transient-receptor-potential, melastatin, 8, cold-temperature, thermosensor, TRPM, 6874, Tocris Bioscience

Citations for AMG 333

Citations are publications that use Tocris products.

Currently there are no citations for AMG 333. Do you know of a great paper that uses AMG 333 from Tocris? Please let us know.

Reviews for AMG 333

There are currently no reviews for this product. Be the first to review AMG 333 and earn rewards!

Have you used AMG 333?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit 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.

Pain

Pain Research Product Guide

A collection of over 280 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.