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AGN 193109

Catalog No. TQ0097 CAS 171746-21-7

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).

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AGN 193109, CAS 171746-21-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 62.00
2 mg	In stock	$ 92.00
5 mg	In stock	$ 155.00
10 mg	In stock	$ 247.00
25 mg	In stock	$ 498.00
50 mg	In stock	$ 725.00
100 mg	In stock	$ 987.00
1 mL * 10 mM (in DMSO)	In stock	$ 198.00

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Purity: 99.89%

Purity: 98.81%

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Description	AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ).
Targets&IC50	RARβ:2 nM (Kd), RARγ:3 nM (Kd), RARα:2 nM (Kd)
In vitro	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 increases in levels of K7, K8, and K19 [2].
In vivo	Topical administration of AGN 193109 at doses of 0.30 or 1.20 μmol/kg significantly mitigates weight loss and cutaneous toxicity associated with concurrent oral TTNPB treatment. A dose of 1.15 μmol/kg AGN 193109 exhibits no apparent toxicity and does not influence spleen weight in mice, yet effectively inhibits the TTNPB-induced spleen weight increase. Furthermore, AGN 193109 notably attenuates ATRA-induced cutaneous toxicity.
Cell Research	Cells (10,000/cm2) are seeded in complete medium and allowed to attach overnight. The cells are then shifted to defined medium (DM), allowed to equilibrate for 24 h, and treatment is initiated by the addition of fresh DM or DM containing epidermal growth factor (EGF) or retinoid. After 3 days of daily treatment with retinoid, the cells are harvested with 0.025% trypsin, 1 mM EDTA, fixed in isotonic buffer containing 4% formaldehyde, and counted using a counter [2].
Animal Research	Mice (n=6) are treated topically on the dorsal skin with vehicle (92.5% acetone/7.5% DMSO), 0.072 μmol/kg of TTNPB, 1.15 μmol/kg of AGN 193109, or 0.072 μmol/kg of TTNPB plus 0.072, 0.288, or 1.15 μmol/kg of AGN 193109 for 5 days. Mice are euthanized on Day 8 [3].

Molecular Weight	392.49
Formula	C28H24O2
CAS No.	171746-21-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.92 mg/mL (10 mM)

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library NO PAINS Compound Library Metabolism Compound Library Neuronal Differentiation Compound Library Bioactive Compounds Library Max Autophagy Compound Library Bioactive Compound Library Nuclear Receptor Compound Library Anti-Metabolism Disease Compound Library Lipid Metabolism Compound Library

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Keywords

AGN 193109 171746-21-7 Autophagy Metabolism Retinoid Receptor Inhibitor Retinoic acid receptors Retinoid X receptors RAR/RXR AGN193109 inhibit AGN-193109 inhibitor

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