AGN 193109 (sodium salt)

AGN 193109 sodium is the sodium salt form of AGN 193109 (HY-U00449). AGN 193109 sodium is the pan antagonist for retinoic acid receptor (RAR), with Kd of 2, 2 and 3 nM, for RARα, RARβ and RARγ, respectively. AGN 193109 sodium reverses TTNPB-induced morphology changes and all-trans retinoic acid (tRA)/9-cis RA/13-cis RA-induced proliferation suppression in ECE16-1 cell. AGN 193109 sodium is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity[1][2].

RXR α: 2 nM (Kd); RXR β: 2 nM (Kd); RXR γ: 2 nM (Kd)

[1] Standeven AM, et al. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol. 1996 May;138(1):169-75. DOI:10.1006/taap.1996.0110
[2] Agarwal C, et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem. 1996 May 24;271(21):12209-12. DOI:10.1074/jbc.271.21.12209