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Submit ReviewA 425619
Description: Potent TRPV1 antagonist
Chemical Name: N-5-Isoquinolinyl-N'-[[(4-(trifluoromethyl)phenyl]methyl]urea
Purity: ≥98% (HPLC)
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 |
| 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.
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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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 for A 425619
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
If you know of a relevant reference for A 425619, please let us know.
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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:
Jong-Woo et al (2022) Melanocortin-4 receptors activate sympathetic preganglionic neurons and elevate blood pressure via TRPV1. Cell Rep 41 111579 PMID: 36323255
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
Do you know of a great paper that uses A 425619 from Tocris? Please let us know.
Reviews for A 425619
Average Rating: 4 (Based on 1 Review.)
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Inhibiting calcium entry in human mast cells stimulated with cortistatin.
By
ANANTH KUMAR KAMMALA on 01/30/2021
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.
