AGN 193109
Biochem/physiol Actions
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.
| Colour | white to beige |
|---|---|
| InChI key | NCEQLLNVRRTCKJ-UHFFFAOYSA-N |
| InChI | 1S/C28H24O2/c1-19-4-11-22(12-5-19)24-16-17-28(2,3)26-15-10-21(18-25(24)26)7-6-20-8-13-23(14-9-20)27(29)30/h4-5,8-16,18H,17H2,1-3H3,(H,29,30) |
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | −20°C |
| Solubility | DMSO: 2 mg/mL, clear (warmed) |
| Form | powder |
| Assay | ≥98% (HPLC) |
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