Potent RXR antagonist (IC50= 18 nM). Promotes white and brown pre-adipocyte differentiation into white adipocytes. Also inhibitsbexarotene-induced brown adipogenic reprogramming of myoblasts.
1.Ebisawa M, Umemiya H, Ohta K, Fukasawa H, Kawachi E, Christoffel G, Gronemeyer H, Tsuji M, Hashimoto Y, Shudo K et al.. (1999) Retinoid X receptor-antagonistic diazepinylbenzoic acids.. Chem Pharm Bull, 47 (12):(1778-86). [PMID:10748721][10.1021/op500134e]
2.Sakaki J, Konishi K, Kishida M, Gunji H, Kanazawa T, Uchiyama H, Fukaya H, Mitani H, Kimura M. (2007) Synthesis and structure-activity relationship of RXR antagonists based on the diazepinylbenzoic acid structure.. Bioorg Med Chem Lett, 17 (17):(4808-11). [PMID:17651969][10.1021/op500134e]
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