FXR

NR1H4 activator 1 is a highly selective agonist of the Farnesoid X Receptor (FXR), demonstrating exceptional FXR activation with an EC50 value of 1 nM in human assays. This compound has been identified for its potential therapeutic applications in gastrointestinal diseases. Its potent activity makes it a valuable tool for research focused on metabolic regulation and liver health.

Danifexor is a selective agonist of the farnesoid X receptor (FXR), which plays a crucial role in regulating bile acid, lipid, and glucose metabolism. Its activation of FXR is associated with beneficial effects on metabolic disorders and liver diseases. Danifexor is utilized in research exploring therapeutic avenues for conditions such as non-alcoholic fatty liver disease (NAFLD) and hyperlipidemia.

Hedragonic acid is an oleane-type triterpenoid that acts as a potent agonist for the farnesoid X receptor (FXR). This compound has demonstrated protective effects against liver damage induced by acetaminophen overdose and is effective in reducing liver inflammation. Hedragonic acid is valuable for research focused on liver health, metabolic disorders, and the modulation of bile acid homeostasis.

FXR Agonist 12 is a selective agonist for the farnesoid X receptor (FXR). It effectively down-regulates genes associated with bile acid synthesis while up-regulating those involved in bile acid transport in HepG2 cells. In preclinical studies, FXR Agonist 12 has demonstrated the capability to improve cholestasis induced by ANIT and to mitigate liver damage and fibrosis in mouse models of non-alcoholic steatohepatitis (NASH). This compound is instrumental for research focusing on liver disorders and bile acid metabolism.

Alismanol M is a farnesoid X receptor (FXR) agonist, exhibiting an EC50 value of 50.25 μM. This protostane-type triterpenoid, derived from the rhizome of Alisma orientale, plays a significant role in modulating bile acid homeostasis. Alismanol M is valuable for research into cholestasis and nonalcoholic steatohepatitis, providing insights into liver metabolism and disease mechanisms.

LZ-007 is a highly selective agonist of the farnesoid X receptor (FXR), exhibiting an EC50 of 51 nM in TR-FRET assays and 76 nM in HepG2 cells. This compound demonstrates favorable pharmacokinetic properties in SD rats. LZ-007 has shown efficacy in ameliorating metabolic dysfunction associated with steatohepatitis in models of western diet and CCl4-induced mice, making it a valuable tool for research in metabolic diseases and liver dysfunction.

XJ02862-S2 is a potent agonist of the farnesoid X receptor (FXR). It demonstrates significant biological activity and holds promise as a lead compound in research focused on non-alcoholic fatty liver disease (NAFLD). XJ02862-S2 may serve as a valuable tool for elucidating the role of FXR in metabolic disorders and developing therapeutic strategies for liver-related diseases.

Ferolin is an agonist of the farnesoid X receptor (FXR), exhibiting an EC50 of 0.56 µM. This compound effectively inhibits the expression of pro-inflammatory genes, including iNOS, IL-1β, and TNFα, upon FXR activation. Ferolin is valuable for research focused on metabolic regulation, inflammation, and related therapeutic pathways.

FXR Antagonist 2 is a diarylamide derivative that serves as a moderate antagonist of the farnesoid X receptor (FXR). This compound demonstrates potential in the investigation of metabolic disorders, specifically hyperlipidemia and type 2 diabetes. Its ability to modulate FXR activity makes it a valuable tool for exploring therapeutic strategies targeting these conditions.

GSK8062 is a potent agonist of the farnesoid X receptor (FXR), involved in the regulation of bile acid and lipid metabolism. This compound has demonstrated significant biological activity, including the reduction of weight gain and serum glucose levels in preclinical studies. GSK8062 is valuable for research applications related to metabolic disorders and the therapeutic exploration of liver diseases.

2-Oxokolavenol is a selective agonist of the farnesoid X receptor (FXR), demonstrating an EC50 of approximately 3.7 μM. This compound mitigates acetaminophen-induced hepatocyte damage through an FXR-dependent mechanism, facilitating the recruitment of co-activators and enhancing FXR transcriptional activity. Derived from the plant Aglaia spectabilis, 2-Oxokolavenol is valuable for research on liver diseases and the underlying mechanisms of FXR signaling.

FXR agonist 14 is a selective, orally bioavailable agonist of the farnesoid X receptor (FXR), exhibiting an EC50 of 0.67 nM. This compound demonstrates significant biological activity by alleviating pathological features associated with metabolic syndrome in high-fat and high-sugar diet-induced MASH mice. Additionally, FXR agonist 14 plays a crucial role in exerting protective effects against anti-cholestatic liver disease, making it valuable for research in liver and metabolic disorders.

Fargesone A is a selective agonist of the farnesoid X receptor (FXR). It demonstrates significant anti-inflammatory activity, making it a valuable tool for research in metabolic diseases and inflammatory conditions. This compound is ideal for studies investigating FXR's role in regulating lipid metabolism and inflammation.

FXR Agonist 11 is a selective agonist of the farnesoid X receptor (FXR) with an EC50 of 1.2 μM and a maximum biological effect of 73.7%. This compound significantly elevates glutathione (GSH) levels in liver tissues, making it a valuable tool for investigating mechanisms of drug-induced liver injury and related hepatic disorders. Research applications include studies of metabolic regulation, liver protection, and the modulation of hepatic stress responses.

PX20350 is an FXR (Farnesoid X receptor) agonist, exhibiting EC50 values of 83 nM and 10 nM for mouse and human FXR, respectively. This compound significantly induces the expression of NDRG2 mRNA and demonstrates potent anti-tumor activity by inhibiting the growth and metastasis of liver tumor cells, specifically SK-GI-18. Additionally, PX20350 has been shown to possess anti-tumorigenic effects in orthotopic xenograft mouse models, making it valuable for investigating liver cancer biology and therapeutic strategies.

(E)-GW 4064 is a potent agonist of the farnesoid X receptor (FXR), a nuclear receptor that plays a crucial role in lipid and glucose metabolism. This compound has demonstrated significant biological activity in regulating bile acid synthesis and glucose homeostasis, making it a valuable tool for investigating metabolic disorders. Research applications include studying the effects of FXR activation on metabolic pathways and exploring its potential therapeutic benefits in conditions such as obesity and diabetes.

Fexarine is a potent, non-steroidal selective agonist of the farnesoid X receptor (FXR) with an EC50 of 38 nM. This compound plays a significant role in the regulation of cholesterol and bile acid metabolism. Fexarine is valuable for research applications focusing on metabolic disorders and diseases associated with dysregulated lipid homeostasis.

FXR/CES2 modulator 1 is a dual modulator that functions as an FXR agonist and a CES2 inhibitor. This compound demonstrates significant potential in reducing the intestinal toxicity associated with irinotecan administration. Its unique mechanism of action makes it a valuable tool for research aimed at understanding FXR modulation and its implications in gastrointestinal safety during chemotherapy.

BAR-2227 is a modulator that targets the Farnesoid X Receptor (FXR) as an agonist and inhibits the leukemia inhibitory factor receptor (LIFR). This compound plays a significant role in the investigation of liver fibrosis and associated inflammatory responses. Researchers can utilize BAR-2227 to explore its therapeutic potential in liver diseases and further elucidate underlying mechanisms of fibrosis and inflammation.

Nelumol A is a potent agonist of the farnesoid X receptor (FXR). It is known to regulate bile acid homeostasis, lipid metabolism, and inflammatory responses. Due to its role in metabolic processes, Nelumol A is employed in research studying metabolic disorders, liver diseases, and the pharmacological modulation of FXR pathways.

FXR Agonist 16 is a potent FXR agonist with an EC50 of 2.2 μM, effectively activating FXR transcriptional activity. This compound upregulates small heterodimer partner (SHP) and bile salt export pump (BSEP) while downregulating cytochrome P450 7A1 (Cyp7a1), which contributes to its hepatoprotective properties. FXR Agonist 16 is valuable for research focused on liver injury, demonstrating a reduction in serum AST and ALT levels in models of free fatty acid-induced hepatocellular damage.

FXR Agonist 15 is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 0.76 μM. This compound shows high specificity, exhibiting minimal activation of other nuclear receptors such as LXRα/β, PXR, PPARα/β/γ, and THR-β, with EC50 values greater than 10 μM. FXR Agonist 15 demonstrates the ability to mitigate steatosis, lobular inflammation, hepatocyte ballooning, and liver fibrosis, making it a valuable tool for research into nonalcoholic steatohepatitis (NASH).

Fexarene is a potent and selective nonsteroidal agonist of the Farnesoid X Receptor (FXR), exhibiting an EC50 of 36 nM. This compound plays a crucial role in the regulation of cholesterol and bile acid metabolism, making it valuable for research investigating metabolic disorders and liver function. Fexarene's ability to selectively activate FXR positions it as a significant tool for studying its downstream effects in various biological systems.

ST-1892 is a potent agonist of the farnesoid X receptor (FXR), exhibiting an EC50 value of 7.2 nM. This compound plays a crucial role in studying metabolic inflammation-related diseases and disorders. Its selective activation of FXR allows for exploration of therapeutic strategies targeting metabolic pathways and liver-related conditions.

GSK2324 is a selective agonist of the farnesoid X receptor (FXR), demonstrating an EC50 of 120 nM. This compound is predominantly utilized in diabetes research, where it plays a pivotal role in the modulation of metabolic processes. Pharmacokinetic studies reveal half-life values of 84 minutes in mice, 170 minutes in rats, 110 minutes in beagle dogs, and 120 minutes in cynomolgus monkeys, indicating its potential for translational studies.

5β-Cholane is a potent activator of the farnesoid X receptor (FXR). It plays a critical role in regulating bile acid homeostasis and lipid metabolism, making it a valuable tool for investigating cholesterol and lipid-related disorders. Researchers can utilize 5β-Cholane to better understand the molecular mechanisms underlying metabolic diseases and to explore therapeutic interventions targeting FXR.

FXR agonist 9 is a selective partial agonist of the farnesoid X receptor (FXR) with an EC50 of 0.09 µM, exhibiting 75.13% maximum efficacy. This compound has demonstrated the ability to improve pathological features associated with metabolic dysfunction and steatohepatitis in mouse models induced by a high-fat diet and carbon tetrachloride. FXR agonist 9 is valuable for research into metabolic disorders and liver diseases.

FXR antagonist 3 is a selective antagonist of the farnesoid X receptor (FXR) with an IC50 of 0.89 μM. This compound exhibits notable activity in modulating intestinal FXR signaling pathways, making it valuable for research related to metabolic disease and bile acid regulation. It serves as a useful tool in studying the physiological roles of FXR in gastrointestinal disorders and potential therapeutic interventions.

sEH/FXR-IN-1 is a selective ligand for soluble epoxide hydrolase (sEH) and the farnesoid X receptor (FXR). This compound demonstrates biological activity by modulating sEH enzymatic activity and influencing FXR signaling pathways. It is utilized in research related to metabolic disorders, inflammation, and liver disease, offering potential insights into therapeutic strategies targeting these pathways.

Tauro-α-muricholic acid (T-α-MCA) is a conjugated bile acid that acts as an antagonist of the farnesoid X receptor (FXR), exhibiting an IC50 of 28 µM. This compound is instrumental in modulating FXR signaling pathways, particularly in the context of bile acid activation. Its research applications include investigations into Alzheimer's disease, as well as studies on glucose and lipid metabolism.

3-Epideoxycholic acid is a modulator of the Farnesoid X receptor (FXR), primarily influencing dendritic cell function. This compound reduces the immunostimulatory capacity of dendritic cells, facilitating the generation of regulatory T cells (Tregs) and exhibiting notable anti-inflammatory effects. Additionally, 3-Epideoxycholic acid promotes the growth of beneficial gut bacteria, specifically Bacteroides, making it relevant for research in immunology and microbiome studies.

Isochenodeoxycholic acid (isoCDCA) is a potent farnesoid X receptor (FXR) agonist. It effectively activates FXR and enhances the mRNA expression of target genes such as Ostβ and Kng1. Isochenodeoxycholic acid is also a substrate for the liver class I ADH γγ isozyme, facilitating the 3β-dehydrogenation reaction. This compound is valuable for research in metabolic processes and FXR-related signaling pathways.

Tauro-α-muricholic acid sodium is a sodium salt of a taurine-conjugated primary bile acid that functions as an antagonist of the farnesoid X receptor (FXR) with an IC50 of 28 µM. This compound effectively inhibits FXR signaling mediated by other bile acids. Research applications include studies on Alzheimer's disease, glucose metabolism, and lipid metabolism, providing valuable insights into metabolic regulation and related disorders.