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A-1120 is a non-retinoid retinol binding protein 4 (RBP4) antagonist (Ki = 8.3 nM for disruption of RBP4 binding to transthyretin).1 It is selective for RBP4 over cellular retinol binding protein 1 (CRBP1; IC50s = 0.09 and >30 µM, respectively, in radioligand binding assays), as well as a panel of G protein-coupled receptors, kinases, and enzymes. A-1120 (30 mg/kg) reduces serum levels of RBP4 and retinol in mice. It also inhibits retinal bisretinoid accumulation in the Abca4-/- mouse model of enhanced retinal lipofuscinogenesis-induced macular degeneration.2
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1. Identification and characterization of a non-
2. A1120, a nonretinoid RBP4 antagonist, inhibits formation of cytotoxic bisretinoids in the animal model of enhanced retinal lipofuscinogenesis. Invest. Ophthalmol. Vis. Sci. 54(1), 85-95 (2013).