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Submit ReviewAMG 333
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)
Biological Activity for AMG 333
AMG 333 is a 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.
Compound Libraries for AMG 333
AMG 333 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for AMG 333
| 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 for AMG 333
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.33 | 100 | |
| ethanol | 45.33 | 100 |
Preparing Stock Solutions for AMG 333
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 |
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Product Datasheets for AMG 333
References for AMG 333
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.
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Keywords: AMG 333, AMG 333 supplier, AMG333, Potent, selective, TRPM8, antagonists, antagonism, transient-receptor-potential, melastatin, 8, cold-temperature, thermosensor, TRPM, 6874, Tocris Bioscience
1 Citation for AMG 333
Citations are publications that use Tocris products. Selected citations for AMG 333 include:
Michael D et al (2023) Nebulized Menthol Impairs Mucociliary Clearance via TRPM8 and MUC5AC/MUC5B in Primary Airway Epithelial Cells. Int J Mol Sci 24 PMID: 36675209
Do you know of a great paper that uses AMG 333 from Tocris? Please let us know.
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