Biological Activity
Potent TRPM8 antagonist (IC50 values are 0.8, 3.0 and 4.4 nM for canine, human and rat channels respectively). Exhibits antiallodynic properties in pain models in vivo.
Compound Libraries
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Technical Data
M. Wt | 467.41 |
Formula | C23H19F6N3O |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 1221349-53-6 |
PubChem ID | 45274257 |
InChI Key | GZINXHRSQAMEQY-ZZEZOPTASA-N |
Smiles | FC(C(C=CC=C3)=C3C1=CC(C(F)(F)F)=C(NC(C4=NOC5(CCCCC5)C4)=N2)C2=C1)(F)F |
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 | 46.74 | 100 | |
ethanol | 46.74 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 467.41. 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.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.14 mL | 10.7 mL | 21.39 mL |
5 mM | 0.43 mL | 2.14 mL | 4.28 mL |
10 mM | 0.21 mL | 1.07 mL | 2.14 mL |
50 mM | 0.04 mL | 0.21 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Parks et al (2011) Design and optimization of benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonists. J.Med.Chem. 54 233 PMID: 21128593
Keywords: TC-I 2014, supplier, TC-I2014, TRPM8, antagonist, TRPM, TRPM, Tocris Bioscience