RG-239 is an orally active TGR5 agonist with an EC50 of 120 nM, significantly more potent than Betulinic acid (EC50= 1.04 µM). It exhibits much higher selectivity for TGR5 over FXRalpha. The compound enhances mitochondrial activity in adipocytes and promotes neurite outgrowth at higher concentrations. Additionally, RG-239 inhibits LPS-induced iNOS expression and nitrite production in Raw264.7 cells and microglia. RG-239 is applicable for research related to type 2 diabetes.
Molekulargewicht:
496.76
CAS Nummer:
[1199222-56-4]
Formel:
C33H52O3
Target-Kategorie:
GPCR19
T211831
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