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].

Product Specifications

CAS Number

[1199222-56-4]

UNSPSC

12352211

Target

G protein-coupled Bile Acid Receptor 1

Related Pathways

GPCR/G Protein

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Inflammation/Immunology

Smiles

OC([C@]12[C@@]([C@@H](CC2)C(C)=C)([H])[C@]3([H])[C@@](CC1)([C@]4([C@]([C@@]5([C@@](C(C)([C@](O)(CC=C)CC5)C)([H])CC4)C)([H])CC3)C)C)=O

Molecular Formula

C33H52O3

Molecular Weight

496.76

References & Citations

[1]Genet C, et al. Redefining the TGR5 triterpenoid binding pocket at the C-3 position. ChemMedChem. 2010 Dec 3;5 (12) :1983-8. |[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. |[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. |[4]Romero-Ramírez L, et al. Bile acids attenuate PKM2 pathway activation in proinflammatory microglia. Sci Rep. 2022 Jan 27;12 (1) :1459. |[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.