AGN 193109

171746-21-7

C28H24O2

DMSO : 2 mg/mL (5.10 mM; Need warming)

Metabolic Enzyme/Protease

AGN 193109 is a retinoid analog, and acts as a specific and highly effective antagonist of retinoic acid receptors (RARs), with K_ds of 2 nM, 2 nM, and 3 nM for RARalpha, RARbeta, and RARgamma, respectively. IC50 & Target: Kd: 2 nM (RARalpha), 2 nM (RARbeta), 3 nM (RARgamma)^[1] In Vitro: AGN 193109 is a highly effective antagonist of retinoic acid receptors, with K_ds of 2 nM, 2 nM, and 3 nM for RARalpha, RARbeta, and RARgamma, respectively. AGN 193109 is completely RAR specific, because it does not bind to or transactivate through any of the RXRs^[1]. AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist)-dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increase in levels of K7, K8, and K19^[2]. In Vivo: AGN 193109 (1.15 umol/kg) does not causes overt toxicity and has no effect on spleen weight on the mice, but it suppresses TTNPB-induced increase in spleen weight of the mice. AGN 193109 also significantly reduces the cutaneous toxicity induced by ATRA. AGN 193109 (0.30 or 1.20 umol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment^[3].