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.

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.

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

Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).

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

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

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.

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

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.

Danifexor is an agonist of the farnesoid X receptor (Farnesoid X receptor).

5β-Cholane is an activator of the farnesoid X receptor (FXR). It is used in research related to cholesterol and lipid-associated diseases.

Cholic acid 3-O-glucuronide (OCA-3-glucuronide) disodium acts as an agonist for the farnesoid X receptor (FXR) with an EC50 of 91.5 μM. It holds potential for research in bile acid metabolism and detoxification.

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

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

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

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

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

Hyodeoxycholic acid sodium salt, a natural secondary bile acid, enhances high-density lipoprotein function, reduces farnesoid X receptor antagonist bile acids, and induces potent cytotoxicity, apoptosis, and IL-8 synthesis.

(E)-Guggulsterone is an isomer of guggulsterone. As an FXR antagonist, it reduces blood lipids, induces heme oxygenase-1 expression, blocks DENV NS2B/3B activity, and inhibits DENV replication.

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)

Tauro-α-muricholic acid (TαMCA) is an antagonist of the farnesoid X receptor (FXR; IC50 = 28 μM) and a taurine-conjugated form of the murine-specific primary bile acid α-muricholic acid . TαMCA is common in rodents but has also been found in small amounts in human serum.

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

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.