AGN 193109

SKU: orb1219764

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).AGN 193109 is completely RAR specific because it does not bind to or transactivate through any of the RXRs . 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 .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. AGN 193109 (1.15 μmol/kg) does not cause 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.(In Vitro):AGN 193109 (0.1 and 1 μmol/L; 3 w) dose-dependently increases vascular smooth muscle cells (VSMCs) mineralization.AGN 193109 (100 nM; 10 d) induces human pluripotent stem cells (hPSCs) differentiate into olfactory placode cells and neurons.

Key Properties

• CAS Number: 171746-21-7
• MW: 392.49
• Purity: >98% (HPLC)
• Formula: C₂₈H₂₄O₂
• SMILES: Cc1ccc(cc1)C1=CCC(C)(C)c2ccc(cc12)C#Cc1ccc(cc1)C(O)=O
• Target: Retinoid Receptor
• Solubility: DMSO:2 mg/mL (5.10 mM; Need warming)

Bioactivity

• In Vitro:
  AGN 193109 (0.1 and 1 μmol/L; 3 w) dose-dependently increases vascular smooth muscle cells (VSMCs) mineralization. AGN 193109 (100 nM; 10 d) induces human pluripotent stem cells (hPSCs) differentiate into olfactory placode cells and neurons.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Retinoid Receptor