FXR

GW4064 is a selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM).

WAY-362450 is a highly potent, selective, and orally bioavailable farnesoid X receptor (FXR) agonist (EC50: 4 nM, eff=149%).

Lithocholic acid is a bile acid that acts as a detergent to solubilize fats for absorption.

Nidufexor is a farnesoid X receptor (FXR) agonist.

T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively

Cilofexor (GS-9674) is a farnesoid X receptor (FXR) agonist.

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM

DY 268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM).

Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.

Tropifexor, also known as LJN452, is a farnesoid X receptor agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).

PX20606, also known as PX-102, is a FXR agonist. It induces high-density lipoprotein-mediated transhepatic cholesterol efflux in mice and monkeys and prevent atherosclerosis in cholesteryl ester transfer protein transgenic low-density lipoprotein receptor (-/-) mice.

Px-104, also known as Px-102, is a farnesoid X receptor (FXR) agonist potentially for the treatment of non-alcoholic fatty liver disease.

LY2562175 is a potent and selective FXR agonist in vitro and has robust lipid modulating properties, lowering LDL and triglycerides while raising HDL in preclinical species.

AMG-333 is a potent and selective TRPM8 Antagonist.

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.

BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.

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

Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.

Tauro-β-muricholic acid (TβMCA) serves as a competitive and reversible antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 40 μM. This trihydroxylated bile acid demonstrates significant ability to inhibit bile acid-induced hepatocyte apoptosis by preserving mitochondrial membrane potential and hindering FXR signaling. It influences bile acid synthesis, hepatic lipid metabolism, and insulin sensitivity, while its accumulation can disrupt metabolic homeostasis, facilitating cancer stem cell proliferation and tumor progression. TβMCA is valuable in studies related to bile acid metabolism disorders, non-alcoholic fatty liver disease, colorectal cancer, and liver fibrosis, owing to its dual functionality in stabilizing mitochondrial integrity and regulating hepatic metabolism.

EDP-305 is a highly selective agonist of the farnesoid X receptor (FXR), exhibiting potent activity with EC50 values of 34 nM in chimeric FXR and 8 nM in full-length FXR. This compound demonstrates significant antifibrotic effects, making it a valuable tool for studying liver diseases. EDP-305 is relevant in research focused on primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH).

Cilofexor tromethamine is a nonsteroidal agonist of the farnesoid X receptor (FXR), primarily targeting liver diseases. It demonstrates significant potential in improving markers of cholestasis and liver injury, making it a valuable reagent in research for conditions such as primary sclerosing cholangitis. Cilofexor tromethamine has exhibited a favorable safety profile in clinical studies involving patients without cirrhosis, leading to notable enhancements in liver biochemical parameters and cholestatic markers.

F44-A13 is a highly selective antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 value of 1.1 μM. This compound modulates cholesterol metabolism by inducing the expression of CYP7A1, leading to significant reductions in cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in murine models. F44-A13 serves as a valuable tool for investigating metabolic diseases related to lipid dysregulation.

(-)-(E)-Guggulsterone is a natural stereoisomer of Guggulsterone that functions as a Farnesoid X Receptor (FXR) antagonist with an IC50 of 24.06 μM. This compound exhibits significant hypolipidemic effects and demonstrates the ability to suppress dengue virus (DENV) replication by enhancing antiviral interferon responses through the activation of Nrf2 and upregulation of HO-1 expression. Additionally, (-)-(E)-Guggulsterone displays antibacterial properties against various strains, including Bacillus subtilis, Staphylococcus aureus, and Pseudomonas aeruginosa, as well as offering cardiac protective and antioxidant benefits in rat models.

Gly-β-MCA is a potent farnesoid X receptor (FXR) inhibitor, selectively acting within the intestine. This stable bile acid demonstrates significant biological activity, making it a promising candidate for research focused on metabolic disorders. Its oral bioavailability enhances its potential for therapeutic application and further investigation in related studies.

FXR agonist 17 functions as a steroidal agonist of the farnesoid X receptor (FXR), exhibiting EC50 values of 42.2 nM in TR-FRET assays and 176.4 nM in luciferase reporter assays. This compound also activates TGR5 with an EC50 of 2.6 μM while showing no activation of hMRGPRX4. FXR agonist 17 demonstrates significant biological activity through its anti-inflammatory, hepatoprotective, and antifibrotic properties, contributing to the reduction of non-alcoholic steatohepatitis (NAFLD) activity scores and alleviating liver fibrosis severity. It serves as a valuable tool for research into NAFLD, cholestatic liver disease, and liver fibrosis.

Vonafexor is a selective agonist of the farnesoid X receptor (FXR), offering an oral bioavailability profile. This compound has demonstrated substantial reductions in HBsAg levels when used in conjunction with Peg-IFNα. Vonafexor is primarily employed in anti-HBV research, making it a valuable reagent for studies focused on hepatitis B virus therapies.

Ursodeoxycholic acid sodium is a potent agonist of the G-protein coupled receptor 19 (GPCR19) and antagonist of the farnesoid X receptor (FXR). This secondary bile acid plays a crucial role in maintaining intestinal barrier integrity and regulating lipid metabolism. Its ability to modulate bile acid-activated receptors makes it valuable for investigating various hepatic and gastrointestinal diseases. Ursodeoxycholic acid sodium is also orally active, making it suitable for diverse in vitro and in vivo research applications.

Tauro-obeticholic acid is an active metabolite of obeticholic acid, functioning as a potent farnesoid-X receptor (FXR) agonist. This compound exhibits significant biological activity in the regulation of bile acid homeostasis and lipid metabolism. It is primarily utilized in research exploring metabolic disorders, liver diseases, and potential therapeutic interventions targeting FXR pathways.

HPG1860 is a highly selective and potent agonist of the farnesoid X receptor (FXR), demonstrating an EC50 of 18 nM in FXR-luciferase reporter assays. This compound exhibits minimal activity on TGR5 and 13 other related nuclear receptors, with EC50 values exceeding 30.0 μM. HPG1860 is primarily utilized in research investigating non-alcoholic steatohepatitis (NASH) and related metabolic disorders.

BMS-986339 is a potent agonist of the farnesoid X receptor (FXR), demonstrating oral bioactivity. This compound interacts with key residues, including His298 and Asn287, to exert its biological effects. BMS-986339 is utilized in research focusing on primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), making it valuable for studies related to anti-fibrotic pathways.

FXR/HSD17B13 modulator 1 is a potent modulator targeting the farnesoid X receptor (FXR) and hydroxysteroid dehydrogenase 17 beta 13 (HSD17B13). This compound demonstrates significant biological activity relevant to the study of metabolic dysfunction-associated steatohepatitis (MASH). Its modulation of these targets can provide insights into therapeutic strategies for liver-related metabolic disorders.

Deoxycholic acid 3-O-β-D-glucuronide disodium is a potent agonist of the farnesoid X receptor (FXR). This compound has been shown to play a significant role in regulating bile acid homeostasis, lipid metabolism, and glucose metabolism. Its applications include the study of metabolic disorders, liver diseases, and potential therapeutic strategies targeting FXR signaling pathways.

Tauro-β-muricholic acid sodium is a competitive and reversible antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 40 μM. This compound plays a significant role in the modulation of bile acid signaling and is utilized in research applications related to metabolic diseases, liver function, and cholesterol homeostasis. Its ability to inhibit FXR makes it a valuable tool for studying the physiological and pathological roles of bile acids in various biological systems.

FXR Agonist 3 is a potent farnesoid X receptor (FXR) agonist, designed for the treatment of non-alcoholic steatohepatitis (NASH). This compound effectively inhibits the expression of COL1A1, TGF-β1, α-SMA, and TIMP1, showcasing significant anti-fibrogenic properties. Additionally, FXR Agonist 3 markedly reduces liver steatosis and inflammation while improving levels of liver fibrosis, making it a valuable tool in liver disease research.

Arjungenin is a pentacyclic triterpenoid that serves as a potent agoinist of the farnesoid X receptor (FXR). It enhances insulin sensitivity by modulating the functionality of adipocytes, making it relevant for metabolic research. In addition, Arjungenin demonstrates moderate free radical scavenging activity and exhibits inhibitory effects on the growth of Spilarctia obliqua larvae. Its antiviral properties include significant activity against various viruses, notably chikungunya virus (CHIKV).

Chenodeoxycholic acid 3-glucuronide is an active metabolite of Chenodeoxycholic acid that serves as a selective Farnesoid X receptor (FXR) activator, exhibiting an EC50 of 8 μM in in vitro assays. This compound effectively modulates FXR signaling pathways, which are crucial for bile acid homeostasis and lipid metabolism. Research applications include studying metabolic disorders, liver physiology, and the potential therapeutic effects of FXR activation in various disease models.

FXR Antagonist 1 is a selective antagonist of the farnesoid X receptor (FXR) with an IC50 of 2.1 μM. This compound effectively inhibits intestinal FXR signaling, promoting feedback activation of hepatic FXR. Its primary biological activity involves ameliorating hepatic steatosis, inflammation, and fibrosis in models of nonalcoholic steatohepatitis (NASH). FXR Antagonist 1 is a valuable tool for research focused on NASH and related metabolic disorders.

Omesdafexor is a potent FXR agonist characterized by its unique non-bile acid structure, demonstrating efficacy in modulating bile acid and lipid metabolism. This compound is particularly relevant for research in non-alcoholic steatohepatitis (NASH), offering insights into therapeutic strategies for metabolic liver diseases. Its oral bioactivity facilitates its application in in vivo studies, making it a valuable tool for investigating FXR-related pathways in liver health and disease.

Linafexor is a potent FXR ( Farnesoid X Receptor) agonist that modulates bile acid homeostasis. By activating FXR, it plays a crucial role in regulating liver function. This compound is particularly relevant for research on primary sclerosing cholangitis (PSC) and metabolic dysfunction-associated steatohepatitis (MASH), offering insights into therapeutic strategies for liver-related diseases.

ZLY28 is a first-in-class dual modulator targeting farnesoid X receptor (FXR) and fatty acid-binding protein 1 (FABP1). This orally active compound exhibits significant potential as an anti-NASH agent, making it a valuable tool for research into nonalcoholic steatohepatitis (NASH) and related metabolic conditions. Its intestinal-restricted activity highlights its specificity, providing an innovative approach to studying lipid metabolism and liver function.

V023-9340 is a potent antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 4.27 μM. This compound is a valuable tool for investigating the role of FXR in the pathology of nonalcoholic steatohepatitis (NASH) and other related metabolic disorders. Its inhibitory action allows for the exploration of FXR's involvement in lipid metabolism and inflammation pathways, making it useful in therapeutic research targeting these conditions.

Glyco-Obeticholic acid is an active metabolite of Obeticholic acid and acts as a farnesoid X receptor (FXR) agonist. By activating FXR, it plays a vital role in regulating bile acid homeostasis, lipid metabolism, and glucose metabolism. This compound is primarily used in research to investigate metabolic disorders, liver diseases, and potential therapeutic strategies for cholestatic liver conditions.

FXR Agonist 5 functions as a selective agonist for the farnesoid X receptor (FXR). This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research on metabolic disorders characterized by inflammation. Its application extends to studying the role of FXR in regulating bile acid homeostasis and glucose metabolism, thus providing insights into potential therapeutic strategies for related diseases.

NDB is a selective antagonist of the human farnesoid X receptor alpha (hFXRα), serving to modulate the transcription of downstream genes associated with this pathway. This compound demonstrates potential in anti-diabetic research by influencing metabolic processes regulated by FXRα. Its application is particularly relevant for studies investigating the role of bile acids and metabolism in diabetes and related disorders.

HEC96719 is a selective tricyclic agonist of the farnesoid X receptor (FXR) that demonstrates potent activity with EC50 values of 1.37 nM and 1.55 nM in time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. This compound has shown significant efficacy in improving non-alcoholic steatohepatitis (NASH) and liver fibrosis, exhibiting favorable distribution in liver and intestinal tissues. HEC96719 is valuable for research focusing on non-alcoholic steatohepatitis and related liver conditions.

Cholic acid 3-O-glucuronide disodium is an agonist of the farnesoid X receptor (FXR), exhibiting an EC50 value of 91.5 μM. This compound plays a significant role in the study of bile acid metabolism and detoxification processes. It is a valuable reagent for research applications focused on liver function and metabolic regulation.

FXR agonist 4 is an agonist of the farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. It demonstrates significant efficacy in ameliorating hyperlipidemia, hepatic steatosis, insulin resistance, and hepatic inflammation in dietary-induced obesity (DIO) mouse models. This compound is valuable for research focused on non-alcoholic fatty liver disease (NAFLD) and its associated metabolic disorders.

β-FXR antagonist 1 is a selective antagonist of the Farnesoid X receptor (FXR), a key regulator of bile acid and lipid metabolism. This compound has demonstrated biological activity in inhibiting FXR-mediated signaling pathways, making it valuable for research focused on metabolic diseases and liver function. Its application spans studies on cholesterol homeostasis, insulin sensitivity, and potential therapeutic interventions in conditions such as non-alcoholic fatty liver disease (NAFLD).

BMS-986318 is a potent non-bile acid agonist of the farnesoid X receptor (FXR), exhibiting EC50 values of 53 nM and 350 nM in FXR Gal4 and SRC-1 recruitment assays, respectively. This compound possesses a favorable ADME profile and has demonstrated efficacy in preclinical models of liver cholestasis and fibrosis, particularly in mouse bile duct ligation studies. BMS-986318 is suitable for research related to nonalcoholic steatohepatitis and its potential therapeutic implications.