A 425619

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Description: Potent TRPV1 antagonist
Chemical Name: N-5-Isoquinolinyl-N'-[[(4-(trifluoromethyl)phenyl]methyl]urea
Purity: ≥98% (HPLC)
Citations (2)
Reviews (1)

Biological Activity for A 425619

A 425619 is a 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.

Compound Libraries for A 425619

A 425619 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for A 425619

M. Wt 345.32
Formula C18H14F3N3O
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 581809-67-8
PubChem ID 8068410
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for A 425619

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 34.53 100
ethanol 34.53 100

Preparing Stock Solutions for A 425619

The following data is based on the product molecular weight 345.32. Batch specific molecular weights may vary from batch to batch due to the degree 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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References for A 425619

References are publications that support the biological activity of the product.

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, A 425619 supplier, A425619, TRPV1, antagonists, antagonism, transient, receptor, potential, channels, vanilloids, pain, nociception, capsaicin, TRPV, 5781, Tocris Bioscience

2 Citations for A 425619

Citations are publications that use Tocris products. Selected citations for A 425619 include:

Chakrabarti et al (2018) Acute inflammation sensitizes knee-innervating sensory neurons and decreases mouse digging behavior in a TRPV1-dependent manner. Neuropharmacology 143 49 PMID: 30240782

Jong-Woo et al (2022) Melanocortin-4 receptors activate sympathetic preganglionic neurons and elevate blood pressure via TRPV1. Cell Rep 41 111579 PMID: 36323255

Do you know of a great paper that uses A 425619 from Tocris? Please let us know.

Reviews for A 425619

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Inhibiting calcium entry in human mast cells stimulated with cortistatin.
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: LAD2 - mast cells

A425619 product was used to study the role of MrgprX2 receptor in calcium mobilization in human mast cells. At a concentration of 0.01 and 0.03uM A425619 inhibited calcium entry significantly when stimulated mast cells with cortistatin.

PMID: 32038646 Reference
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