retinoid action

Tazarotenic acid (AGN-190299) is a retinoid prodrug which is converted to its active form

11-cis Retinol is an isomer of vitamin A, serving as an agonist for red rod optochromin and an inverse agonist for red cone optochromin.

AGN-190121 is a retinoic acid receptor (RAR) agonist. RAR and Retinoid X Receptor (RXR) ligands can act synergistically to induce hypertriglyceridemia through distinct mechanisms of action.

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; Kd= 2, 2, and 3 nM for RARα, β, and γ, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs; Kd= >10,000 nM for human RXRα, β, and γ receptors). This compound effectively reverses cellular morphology changes and growth suppression induced by RAR agonists such as all-trans-RA, 13-cis-RA, and 9-cis-RA in ECE16-1 human endometrial ectocervical epithelial cells, particularly when used at a 10-fold molar excess. Furthermore, AGN 193109 downregulates the expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, indicating inhibition of retinoid action, specifically when co-administered with TTNPB but not as a standalone treatment. In vivo studies demonstrate teratogenic effects, including cleft palate, frontonasal dysplasia, and eye malformations in mouse fetuses following a single oral dose of 1 mg/kg.