AGN 193109 is an orally active retinoic acid receptor (RAR) antagonist that targets all three RAR subtypes with higher affinity (RARα/β/γ Kd = 2 nM) than all-trans retinoic acid/ATRA (RARα/β/γ Kd = 9/12/19 nM). AGN 193109 potently antagonizes against ATRA-induced transcription in RARα, RARβ, and RARγ transfected CV-1 cells (by 85%, 62%, and 100%, respectively, by equal molar AGN 193109 against ATRA). AGN 193109 is also widely employeed to block RAR-mediated physiological and pathalogical processes in mice and rats in vivo via oral (1-10 mg/kg) or topical (0.3-36 μmol/kg) administration.
Neuroblastoma is the most common inheritable, solid neoplasm in children found under the age of 7 and accounts for approximately 7% of childhood cancers. A common treatment that has been prescribed for over a decade is retinoid therapy [using all‑trans
Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors.
A T Johnson et al.
Journal of medicinal chemistry, 38(24), 4764-4767 (1995-11-24)
Proceedings of the National Academy of Sciences of the United States of America, 113(50), 14354-14359 (2016-12-03)
The Müllerian duct develops into the oviduct, uterus, and vagina, all of which are quite distinct in their morphology and function. The epithelial fate of these female reproductive organs in developing mice is determined by factors secreted from the stroma;
Toxicology and applied pharmacology, 138(1), 169-175 (1996-05-01)
AGN 193109 was recently identified as a potent retinoic acid receptor (RAR) antagonist in vitro. The purpose of the present study was to determine if AGN 193109 functions as an RAR antagonist in vivo and thus could prevent and/or treat
A series of high affinity retinoic acid receptor (RAR) antagonists were prepared based upon the known antagonist AGN 193109 (2). Introduction of various phenyl groups revealed a preference for substitution at the para-position relative to the meta-site. Antagonists with the
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
