RG-239 is an orally active TGR5 agonist with an EC 50 of 120 nM, significantly outperforming Betulinic acid ( HY-10529 ) ( EC 50 = 1.04 μM). RG-239 demonstrates higher selectivity for TGR5 compared to the FXRα. RG-239 increases mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. RG-239 inhibits LPS ( HY-D1056 )-induced iNOS expression and nitrite production in Raw264.7 and microglia cells. RG-239 can be used for the study of type 2 diabetes [1][2][3][4][5] .
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