A 425619

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Cat.No. 5781 - A 425619 | C18H14F3N3O | CAS No. 581809-67-8
Description: Potent TRPV1 antagonist
Chemical Name: N-5-Isoquinolinyl-N'-[[(4-(trifluoromethyl)phenyl]methyl]urea
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent TRPV1 antagonist (IC50 = 3-9 nM). Blocks capsaicin-evoked currents in rat DRG neurons and inhibits TRPV1-activation by anandamide (Cat. No. 1339) and N-arachidonoyl-dopamine. Reduces pain in inflammatory, postoperative and osteoarthritic in vivo pain models.

Technical Data

M. Wt 345.32
Formula C18H14F3N3O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 581809-67-8
PubChem ID 8068410
InChI Key SJGVXVZUSQLLJB-UHFFFAOYSA-N
Smiles O=C(NCC1=CC=C(C(F)(F)F)C=C1)NC2=CC=CC3=CN=CC=C32

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 34.53 100
ethanol 34.53 100

Preparing Stock Solutions

The following data is based on the product molecular weight 345.32. 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 2.9 mL 14.48 mL 28.96 mL
5 mM 0.58 mL 2.9 mL 5.79 mL
10 mM 0.29 mL 1.45 mL 2.9 mL
50 mM 0.06 mL 0.29 mL 0.58 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

El Kouhen et al (2005) A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel and selective transient receptor potential type V1 receptor antagonist, blocks channel activation by vanilloids, heat, and acid. J.Pharmacol.Exp.Ther. 314 400 PMID: 15837819

McGaraughty et al (2006) Systemic and site-specific effects of A-425619, a selective TRPV1 receptor antagonist, on wide dynamic range neurons in CFA-treated and uninjured rats. J.Neurophysiol. 95 18 PMID: 16162831


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Keywords: A 425619, supplier, A425619, TRPV1, antagonists, antagonism, transient, receptor, potential, channels, vanilloids, pain, nociception, capsaicin, TRPV, Tocris Bioscience

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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.

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