FXR Agonist

XJ02862-S2 shows potent FXR agonistic activity. XJ02862-S2 is a promising lead compound for the research of NAFLD.

Ferolin is the agonist for farnesoid X receptor (FXR) with an EC₅₀ of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation.

FXR agonist 13 is a selective, orally active, potent FXR agonist (EC₅₀ = 0.097 μM) and has favorable hepatic microsomal metabolic stability. FXR agonist 13 exhibits moderate affinity for FXR-LBD upon direct binding (K_D = 14.74 μM). FXR agonist 13 displays good selectivity against related nuclear receptors, including LXRα/β, PPARα/γ/δ, PXR, and TGR5. FXR agonist 13 can be used for the study of metabolic-associated steatohepatitis (MASH).

2-Oxokolavenol is a selective agonist targeting the farnesoid X receptor (FXR), with an EC₅₀ of ~3.7 μM. 2-Oxokolavenol exerts its activity against Acetaminophen (HY-66005)-induced hepatocyte damage in an FXR-dependent manner by binding to the FXR ligand-binding pocket, recruiting co-activators, and inducing FXR transcriptional activity. 2-Oxokolavenol can be naturally extracted from Aglaia spectabilis (a plant of the Aglaia genus in the Meliaceae family) and can be used in research related to liver diseases.

Cilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis.

FXR agonist 14 (Compound V15) is a partial, selective, orally active FXR agonist with an EC₅₀ of 0.67 nM. FXR agonist 14 ameliorates pathological features in high-fat and high-sugar diet-induced MASH mice. FXR agonist 14 shows significant anti-cholestatic liver disease effects.

FXR agonist 11 (Compound 14) is an FXR agonist with an EC₅₀ of 1.2 μM and a maximum effect of 73.7%. FXR agonist 11 can significantly increase GSH levels in the liver and is used to study drug-induced liver injury diseases.

PX20350 is a FXR agonist with EC₅₀s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.

Tauro 6-ethlchenodeoxycholic acid-d₅ sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.

FXR agonist 17 is an orally active, steroidal FXR agonist with EC₅₀ values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC₅₀ = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis.

(E)-GW 4064 is a FXR agonist.

Fexarine is a potent, non-steroidal and selective agonist of farnesoid X receptor (EC₅₀: 38 nM). Fexarine can be used for the research of diseases linked to cholesterol, bile acids.

Hexanorcucurbitacin D, a cucurbitacin, is a weak ecdysteroid receptor agonist. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD).

BAR-2227 (compound 3a) is a FXR agonist and LIFR inhibitor. BAR-2227 can be used to study liver fibrosis and inflammation.

Nelumol A is a farnesoid X receptor (FXR) agonist.

dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC₅₀ of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model.

FXR agonist 16 is a FXR agonist with an EC₅₀ of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury.

Glyco-obeticholic acid-d₅ is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.

FXR agonist 15 is a selective, potent and orally active farnesoid X receptor (FXR) agonist with EC₅₀ of 0.76 μM. FXR agonist 15 exhibits no obvious activation on other nuclear receptors including LXRα/β, PXR, PPARα/β/γ, THR-β, with EC₅₀ values all >10 μM. FXR agonist 15 can alleviate steatosis, lobular inflammation, hepatocyte ballooning and liver fibrosis. FXR agonist 15 can be used for the research of nonalcoholic steatohepatitis (NASH).

Fexarene is a potent and selective nonsteroidal Farnesoid X Receptor (FXR) agonist with an EC₅₀ of 36 nM. Fexarene can be used in studies of cholesterol and bile acid metabolism.