RXRβ Antagonist

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC₅₀ value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.

LE-540 is a selective retinoic acid receptor antagonist for RARβ (K_i=0.22 μM). LE-540 shows potential for use in cancer research, particularly for breast cancer and lung cancer.

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 K_d 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.