- Cat. No.
- A16077
DY 268
DY 268 is a trisubstituted-pyrazol carboamide based compound that acts as a potent FXR antagonist (IC50 = 7.5 nM).
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- Cat. No.
- A19901
(Z)-Guggulsterone
Synonyms: Z-Guggulsterone
(Z)-Guggulsterone is a phytosteroid found in the resin of the guggul plant, Commiphora mukul. It acts as an antagonist of the farnesoid X receptor in humans.
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- Cat. No.
- A30300
Tauro-β-muricholic acid
Synonyms: TβMCA
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.
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- Cat. No.
- A38882
(-)-(E)-Guggulsterone
Synonyms: (E)-Guggulsterone
(-)-(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.
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- Cat. No.
- A39924
F44-A13
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.
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- Cat. No.
- A69104
FXR/HSD17B13 modulator 1
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.
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- Cat. No.
- A70457
3-Epideoxycholic acid
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.
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- Cat. No.
- A71660
Tauro-α-muricholic acid sodium
Synonyms: T-α-MCA sodium
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.
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- Cat. No.
- A72302
Tauro-α-muricholic acid
Synonyms: T-α-MCA
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.
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- Cat. No.
- A74869
Tauro-β-muricholic acid sodium
Synonyms: T-βMCA sodium
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.
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- Cat. No.
- A74873
FXR antagonist 1
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.
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- Cat. No.
- A74876
ZLY28
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.
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- Cat. No.
- A74878
V023-9340
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.
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- Cat. No.
- A74881
NDB
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.
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- Cat. No.
- A74885
β-FXR antagonist 1
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).
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- Cat. No.
- A74896
FXR antagonist 2
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.
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- Cat. No.
- A74905
FXR/CES2 modulator 1
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.
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- Cat. No.
- A74907
BAR-2227
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.
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- Cat. No.
- A74920
FXR antagonist 3
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.
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