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.
High-affinity orally active pan-retinoic acid receptor (RAR) antagonist with in vitro and in vivo efficacy.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Regulatory Listings
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Proceedings of the National Academy of Sciences of the United States of America, 113(50), 14354-14359 (2016-12-03)
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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)
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