A 784168

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Cat.No. 4319 - A 784168 | C19H15F6N3O3S | CAS No. 824982-41-4
Description: Potent and selective TRPV1 antagonist
Chemical Name: 3,6-Dihydro-3'-(trifluoromethyl)-N-[4-[(trifluoromethyl)sulfonyl]phenyl]-[1(2H),2'-bipyridine]-4-carboxamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent TRPV1 antagonist (IC50 = 25 nM for inhibition of TRPV1 activation by 50 nM capsaicin). Displays no activity against a range of receptors, including TRPA1, GABA, opioid, and purinergic receptors.

Compound Libraries

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Technical Data

M. Wt 479.4
Formula C19H15F6N3O3S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 824982-41-4
PubChem ID 11420211
InChI Key SDUAWRFBHRAFBM-UHFFFAOYSA-N
Smiles O=C(NC3=CC=C(S(=O)(C(F)(F)F)=O)C=C3)C(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 47.94 100
ethanol 23.97 50

Preparing Stock Solutions

The following data is based on the product molecular weight 479.4. 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 2.09 mL 10.43 mL 20.86 mL
5 mM 0.42 mL 2.09 mL 4.17 mL
10 mM 0.21 mL 1.04 mL 2.09 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Bianchi et al (2007) [3H]-A-778317 [1-((R-5-tert-butyl-indan-1-yl)-3-isoquinolin-5-yl-urea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor. J.Pharmacol.Exp.Ther. 323 285 PMID: 17660385

Cui et al (2006) TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists. J.Neurosci. 26 9385 PMID: 16971522


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Citations for A 784168

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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 A 784168

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