AG1529

Overview

AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC 50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus.

Application

Products | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Skin Inflammation | Products > Signaling Pathways > Membrane Transporter/Ion Channel | Products > Signaling Pathways > Neuronal Signaling | Products > Research Areas > Inflammation/Immunology | Products > Signaling Pathways > TRP Channel

Product Information

• Catalog No.: HY-182517
• CAS No.: 2225980-49-2
• Molecular Formula: C22H34INO5
• Molecular Weight: 519.41
• Storage: Please store the product under the recommended conditions in the Certificate of Analysis.

Source

Original product source