AGN 193109 is a potent antagonist of retinoic acid receptors (RARs, Kd= 2, 2, and 3 nM for RARalpha, beta, and gamma, respectively), exhibiting selectivity for RARs over retinoid X receptors (RXRs, Kd= >10,000 nM for human RXRalpha, beta, and gamma 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.
Molekulargewicht:
414.5
CAS Nummer:
[2319838-82-7]
Formel:
C28H23O2?Na
Target-Kategorie:
Others|||Retinoid Receptor
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