JNJ 17203212

Pricing Availability Delivery Time Qty
Cat.No. 3361 - JNJ 17203212 | C17H15F6N5O | CAS No. 821768-06-3
Description: Reversible, competitive and potent TRPV1 antagonist
Chemical Name: 4-[3-(Trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazinecarboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Literature

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.

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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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


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Keywords: JNJ 17203212, supplier, Reversible, competitive, potent, TRPV1, antagonists, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, JNJ17203212, TRPV, Tocris Bioscience

2 Citations for JNJ 17203212

Citations are publications that use Tocris products. Selected citations for JNJ 17203212 include:

Kelly et al (2015) Increased function of pronociceptive TRPV1 at the level of the joint in a rat model of osteoarthritis pain. PLoS One 74 252 PMID: 24152419

Vijayvergiya et al (2015) Measurement of Ensemble TRPV1 Ion Channel Currents Using Droplet Bilayers. PLoS One 10 e0141366 PMID: 26513481


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Literature in this Area

Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.

Pathways for JNJ 17203212

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