AGN 193109 

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 RARα, RARβ, and RARγ, respectively. AGN 193109 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. AGN 193109 is the antidote for retinoic acidosis, that ameliorates the skin and mucosal toxicity.

Kd: 2 nM (RARα), 2 nM (RARβ), 3 nM (RARγ)^[1]

AGN 193109 is a highly effective antagonist of retinoic acid receptors, with K_ds of 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ, 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AGN 193109 (1.15 μmol/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 μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

392.49

C₂₈H₂₄O₂

171746-21-7

Solid

Off-white to light yellow

O=C(O)C1=CC=C(C#CC2=CC=C3C(C)(C)CC=C(C4=CC=C(C)C=C4)C3=C2)C=C1

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Johnson AT, et al. Synthesis and characterization of a highly potent and effective antagonist of retinoic acid receptors. J Med Chem. 1995 Nov 24;38(24):4764-7.  [Content Brief]

  [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.  [Content Brief]

  [3]. Standeven AM, et al. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol. 1996 May;138(1):169-75.  [Content Brief]