RG-239 

RG-239 is an orally active TGR5 agonist with an EC₅₀ of 120 nM, significantly outperforming Betulinic acid (HY-10529) (EC₅₀ = 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]}.

RG-239 (Compound 18 dia 2) (10 μM) 可增强脂肪细胞的线粒体活性，具体表现为 3T3L1 脂肪细胞内细胞色素 C 氧化酶活性的升高^[2]。

RG-239 (1-10 μM) 在 1 μM 浓度下诱导的神经突长度为 9.5 μm，显著低于 Retinoic acid (RA) (HY-14649) 的诱导效果，但在 10 μM 浓度下，其中位神经突长度达到 37.0 μm，与 Deoxycholic acid (DCA) (HY-N0593) 在 NSC-34 细胞中的诱导效果几乎相同^[3]。

RG-239 (2 μM, 24 h) 能够抑制 LPS 诱导的 Raw264.7 和小胶质细胞中 iNOS 表达及亚硝酸盐生成^[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

RG-239 (Compound 18 dia 2) (30 mg/kg/天，口服，3 周) 可降低由 10 周高脂饮食 (脂肪供能占比 60%) 诱导的肥胖小鼠的血浆葡萄糖水平^[2]。

RG-239 (10 mg/kg/天，口服，2 周) 能下调由 10 周高脂饮食 (脂肪供能占比 60%) 诱导的 B6J 小鼠肝脏中炎症基因Tnfα、IL-6 和 IL-1β 的表达^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

496.76

C₃₃H₅₂O₃

1199222-56-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Genet C, et al. Redefining the TGR5 triterpenoid binding pocket at the C-3 position. ChemMedChem. 2010 Dec 3;5(12):1983-8.  [Content Brief]

  [2]. Genet C, et al. Structure-activity relationship study of betulinic acid, a novel and selective TGR5 agonist, and its synthetic derivatives: potential impact in diabetes. J Med Chem. 2010 Jan 14;53(1):178-90.  [Content Brief]

  [3]. Ackerman HD, et al. Bile Acids Induce Neurite Outgrowth in Nsc-34 Cells via TGR5 and a Distinct Transcriptional Profile. Pharmaceuticals (Basel). 2023 Jan 24;16(2):174.  [Content Brief]

  [4]. Romero-Ramírez L, et al. Bile acids attenuate PKM2 pathway activation in proinflammatory microglia. Sci Rep. 2022 Jan 27;12(1):1459.  [Content Brief]

  [5]. Fujisaka S, et al. Antibiotic effects on gut microbiota and metabolism are host dependent. J Clin Invest. 2016 Dec 1;126(12):4430-4443.  [Content Brief]