A TRPV1 antagonist
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

A-425619

Item No. 42117

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-5-isoquinolinyl-N′-[[4-(trifluoromethyl)phenyl]methyl]-urea
CAS Number
581809-67-8
Molecular Formula
C18H14F3N3O
Formula Weight
345.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(NCC1=CC=C(C(F)(F)F)C=C1)NC2=CC=CC3=C2C=CN=C3
InChi Code
InChI=1S/C18H14F3N3O/c19-18(20,21)14-6-4-12(5-7-14)10-23-17(25)24-16-3-1-2-13-11-22-9-8-15(13)16/h1-9,11H,10H2,(H2,23,24,25)
InChi Key
SJGVXVZUSQLLJB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    5 mg

    $149

    Add

    10 mg

    $268

    Add

    25 mg

    $594

    Add

    50 mg

    $966

    Add
    Product Description

    A-425619 is an antagonist of transient receptor potential vanilloid 1 (TRPV1).1 It is selective for TRPV1 over a panel of 83 receptors, enzymes, transporters, and ion channels at 10 µM. A-425619 inhibits increases in intracellular calcium induced by capsaicin (Item No. 92350), N-arachidonoyl dopamine (NADA; Item No. 90057), anandamide (arachidonoyl ethanolamide; Item No. 90050), or acid in HEK293 cells expressing human TRPV1 (IC50s = 5, 4, 3, and 2 nM, respectively). It increases core body temperature in rats when administered at a dose of 30 mg/kg.2 A-425619 increases the paw withdrawal threshold in several rodent models of inflammatory, neuropathic, osteoarthritic, and postoperative pain in a dose-dependent manner.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. El Kouhen, R., Surowy, C.S., Bianchi, B.R., et al. 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(1), 400-409 (2005).

    2. Gavva, N.R., Bannon, A.W., Surapaneni, S., et al. The vanilloid receptor TRPV1 is tonically activated in vivo and involved in body temperature regulation. J. Neurosci. 27(13), 3366-3374 (2007).

    3. Honore, P., Wismer, C.T., Mikusa, J., et al. A-425619 [1-isoquinolin-5-yl-3-(4-trifluoromethyl-benzyl)-urea], a novel transient receptor potential type V1 receptor antagonist, relieves pathophysiological pain associated with inflammation and tissue injury in rats. J. Pharmacol. Exp. Ther. 314(1), 410-421 (2005).