AMG 333

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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

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

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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


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Citations for AMG 333

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