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Submit ReviewAMG 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.
AMG 333 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 453.33 |
公式 | C20H12F5N3O4 |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 45.33 | 100 | |
ethanol | 45.33 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: AMG 333, AMG 333 supplier, AMG333, Potent, selective, TRPM8, antagonists, antagonism, transient-receptor-potential, melastatin, 8, cold-temperature, thermosensor, TRPM, 6874, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 AMG 333 的部分引用包括:
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
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