Biological Activity
Reversible, competitive and potent TRPV1 antagonist (pKi values are 6.5, 7.1 and 7.3 at rat, guinea pig and human TRPV1 respectively). Inhibits capsaicin- and H+-induced channel activation (pIC50 values are 6.32 and 7.23 respectively) and exhibits antitussive and analgesic activity in vivo.
Compound Libraries
JNJ 17203212 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 419.32 |
| Formula | C17H15F6N5O |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 821768-06-3 |
| PubChem ID | 11339118 |
| InChI Key | JFRYYGVYCWYIDQ-UHFFFAOYSA-N |
| Smiles | O=C(NC3=NC=C(C(F)(F)F)C=C3)N(CC2)CCN2C1=C(C(F)(F)F)C=CC=N1 |
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 | 41.93 | 100 | |
| ethanol | 41.93 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 419.32. 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 | 2.38 mL | 11.92 mL | 23.85 mL |
| 5 mM | 0.48 mL | 2.38 mL | 4.77 mL |
| 10 mM | 0.24 mL | 1.19 mL | 2.38 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Swanson et al (2005) Identification and biological evaluation of 4-(3-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid (5-trifluoromethylpyridin-2-yl)amide, a high affinity TRPV1 (VR1) vanilloid receptor antagonist. J.Med.Chem. 48 1857 PMID: 15771431
Ghilardi et al (2005) Selective blockade of the capsaicin receptor TRPV1 attenuates bone cancer pain. J.Neurosci. 25 3126 PMID: 15788769
Bhattacharya et al (2007) Pharmacology and antitussive efficacy of 4-(3-trifluoromethyl-pyridin-2-yl)-piperazine-1-carboxylic acid (5-trifluoromethyl-pyridin-2-yl)-amide (JNJ17203212), a transient receptor potential vanilloid 1 antagonist in guinea pigs. J.Pharmacol.Exp.Ther. 323 665 PMID: 17690251
Keywords: JNJ 17203212, supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, TRPV, TRPV, Tocris Bioscience
