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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
Technical Data for A 425619
|Storage||Store at RT|
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|
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.
|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|
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
1 Citation 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
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Reviews for A 425619
Average Rating: 4 (Based on 1 Review.)
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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.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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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.