farnesoid

Obeticholic Acid (6-ECDCA, INT-747) is a high-affinity, semisynthetic, bile acid-derived FXR agonist with an EC50 of 99 nM and is able to upregulate IκB-α, KLF-2, and KLF-4 expression. Obeticholic Acid (6-ECDCA, INT-747) also shows potential for treating hepatic steatosis, inflammation, and fibrosis while increasing insulin sensitivity.

INT-767 is a potent farnesoid X receptor (FXR) TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.

GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).

Nidufexor is an agonist for the farnesoid X receptor (FXR).

Vonafexor (EYP001) is a farnesoid X receptor (FXR, NR1H4) agonist, with anti-HBV effects

Fexarine is a potent, selective agonist of farnesoid X receptor.

PX20606 is an orally active farnesoid X receptor (FXR) agonist, demonstrating EC50 values of 220 nM (mFXR) and 50 nM (hFXR) in Gal4-FXR assays. It induces the expression of the tumor suppressor gene NDRG2 and inhibits tumor growth and metastasis in a mouse HCC model. Additionally, PX20606 exhibits hepatoprotective properties.

Tauro-obeticholic acid, a farnesoid X receptor (FXR) agonist and semisynthetic derivative of chenodeoxycholic acid, is an active metabolite of obeticholic acid. This compound undergoes taurine conjugation in the liver to form from obeticholic acid and can be reconverted to its original form by intestinal microflora.

HPG1860, an agonist of the farnesoid X receptor (FXR), induces luminescence in reporter gene assays utilizing HEK293T cells expressing human FXR, with an EC50 value of 18 nM. In vivo studies demonstrate that HPG1860 (administered at 1, 3, or 10 mg kg daily) reduces serum alanine aminotransferase (ALT) and total cholesterol levels in a mouse model of non-alcoholic steatohepatitis (NASH), which was induced by a high-fat diet and carbon tetrachloride (CCl4). Additionally, this compound decreases hepatic inflammation, fat levels, and fibrosis.

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

Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).

Fexaramate is a potent, selective agonist of farnesoid X receptor.

Cilofexor, also known as GS-9674, is a farnesoid X receptor (FXR) agonist. The nonsteroidal FXR agonist cilofexor (GS-9674) improves markers of cholestasis and liver injury in patients with PSC. In clinical study, cilofexor was well tolerated and led to significant improvements in liver biochemistries and markers of cholestasis in patients with PSC.

GSK-8062 is an agonist of farnesoid X receptor (FXR).

CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(2020)

Glyco-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an agonist of the farnesoid X receptor (FXR).

TC-G 1005 is a potent and selective GPBA agonist (EC50 :0.72 nM; hTGR5). Selective for TGR5 over FXR (farnesoid X receptor). Increases plasma GLP-1 levels and reduces blood glucose in mice. Orally available.

Vidofludimus hemicalcium (4sc-101; SC12267) is an orally active compound that acts as a dihydroorotate dehydrogenase (DHODH) inhibitor and serves as a novel modulator of the farnesoid X receptor (FXR). This immunomodulatory agent is utilized in the research of autoimmune disorders, including inflammatory bowel disease (IBD), and is explored for its potential in fatty liver disease research through FXR targeting.

Gly-β-MCA is an orally bioactive, enteroselective and potent inhibitor of the farnesoid X receptor (FXR), a bile acid, used in the study of obesity and diabetes.

Lecufexor is an agonist of the farnesoid X receptor (FXR).

LZ-007 is an agonist of the Farnesoid X receptor (FXR), with an EC50 of 51 nM as determined by TR-FRET assay, and an EC50 of 76 nM in HepG2 cells. It exhibits favorable pharmacokinetic properties in SD rats and can improve metabolic dysfunction-associated steatohepatitis induced by high-fat diets and CCl4 in mice.

Androsterone, a metabolic product of testosterone, can activate Farnesoid X Receptor (FXR).