PX20606 trans racemate is a FXR agonist with EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.
FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation[1].
INT-767 is a dual farnesoid X receptor/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
(-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
Sevelamer Hcl is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
Nidufexor is a farnesoid X receptor (FXR) agonist[1].
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds. IC50 value:Target:in vitro: In vitro treatment of CDCA or fexaramine elevated the SHP transcript level and occupancy on secretin promoter [1]. Fexaramine significantly enhanced osteoblastic differentiation through the upregulation of Runx2 and enhanced extracellular signal-regulated kinase (ERK) and β-catenin signaling [2]. By mimicking this tissue-selective effect, the gut-restricted FXR agonist fexaramine (Fex) robustly induces enteric fibroblast growth factor 15 (FGF15), leading to alterations in BA composition, but does so without activating FXR target genes in the liver [3].
Nelumol A is a farnesoid X receptor (FXR) agonist[1].
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[1].
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].
INT-747 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active[1][2].
GW 4064 is a potent FXR agonist with EC50 of 65 nM.
WAY-362450 is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease[1].
BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis[1].
GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively[1].
T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively.
Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist[1].
Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist[1].
Omesdafexor is a FXR agonist. Omesdafexor can be used in the research of liver disease or a metabolic inflammation-mediated disease[1][2].
Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation[1].
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential[1][2].
Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis[1].
FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the treatment of fatty liver disease.
β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist[1].