AGN 193109 (sodium salt)

AGN 193109 is a potent antagonist of retinoic acid receptors (RARs; K_d = 2, 2, and 3 nM for RARα, β, and γ, respectively).¹ It is selective for RARs over retinoid X receptors (RXRs; K_d = >10,000 nM for human RXRα, β, and γ receptors). AGN 193109 reverses changes in cell morphology induced by the RAR agonist TTNPB (Item No. 16144) in ECE16-1 human endometrial ectocervical epithelial cells. It also reverses the growth suppressive effects of all-trans-RA, 13-cis-RA, and 9-cis-RA (Item No. 14587) when used at a 10-fold molar excess. AGN 193109 decreases expression of cytokeratin K5-8, 13, 14, 16, 17, and 19 genes, markers of retinoid action in ECE16-1 cells, when co-administered with TTNPB but not when used alone. In vivo, AGN 193109 induces cleft palate or frontonasal dysplasia and eye malformations in fetuses of pregnant mice following a single oral dose of 1 mg/kg.²

WARNING This product is not for human or veterinary use.

1. Agarwal, C., Chandraratna, A.S., Johnson, A.L., et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. The Journal of Biological Chemisty 271(21), 12209-12212 (1996).

2. Kochhar, D.M., Jiang, H., Penner, J.D., et al. The use of a retinoid receptor antagonist in a new model to study vitamin A-dependent developmental events. Int. J. Dev. Biol. 42(4), 601-608 (1998).