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V-125 is an agonist of retinoid X receptors (RXRs).1 It induces homodimerization of RXR in HCT116 cells in a two-hybrid assay (EC50 = 13.8 nM). V-125 selectively induces transactivation of RXRα in human RXRα-overexpressing HCT116 cells over transactivation of RARα in human RARα-overexpressing HEK293 cells when used at concentrations of 25 and 100 nM, respectively. In vivo, V-125 (80 mg/kg in the diet) inhibits vinyl carbamate-induced lung tumor growth in mice.2 Unlike the RXR agonist bexarotene (Item No. 11571), V-125 does not increase plasma triglyceride or cholesterol levels in mice.
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1. Modeling, synthesis, and biological evaluation of potential retinoid X receptor (RXR)-
2. The rexinoid V‑125 reduces tumor growth in preclinical models of breast and lung cancer. Sci. Rep. 12(1), 293 (2022).