TR-14035

TR-14035 (CAS No.: 232271-19-1) is a potent, orally active small-molecule dual antagonist of α4β7 and α4β1 integrins, key adhesion receptors involved in leukocyte trafficking and inflammatory responses, positioning it as a valuable tool compound in immunology and inflammation research. It exhibits high affinity inhibition of α4β7 and α4β1 integrins in the nanomolar range, and effectively disrupts integrin-mediated cell adhesion processes, including the interaction between α4β7-expressing lymphoid cells and mucosal addressin cell adhesion molecule-1, as well as fibronectin connecting segment 1-induced adhesion in relevant cell systems. Through blockade of these integrin pathways, TR-14035 interferes with leukocyte adhesion and migration under both static and shear flow conditions, highlighting its relevance to studies of immune cell homing and tissue-specific inflammation. In vitro and cellular assays typically demonstrate activity spanning nanomolar to low micromolar concentrations depending on the model system, while in vivo studies in rodent models of allergic inflammation have shown that administration of the compound can attenuate airway hyperresponsiveness, supporting its utility in investigating integrin-driven mechanisms in asthma and other inflammatory or autoimmune disorders. Experimental concentrations or dosing regimens vary according to specific study designs and therapeutic hypotheses, making TR-14035 broadly applicable for mechanistic studies, target validation, and preclinical drug discovery efforts focused on integrin-mediated signaling pathways.