574013-66-4

Usage

Uses

Used in Pharmaceutical Research:
Fexaramine is used as a pharmaceutical agent for studying its action on RANKL (receptor activator of nuclear factor-κB ligand)-induced osteoclastogenesis in mouse models. This application is significant for understanding the role of FXR agonists in bone metabolism and potential therapeutic interventions for related conditions.
Used in Cholesterol and Lipid Metabolism:
As an FXR agonist, Fexaramine is used in the study and regulation of cholesterol metabolism and lipid homeostasis. Its high affinity and potency for FXR make it a valuable tool for investigating the role of FXR in these processes and for developing potential treatments for dyslipidemia and related metabolic disorders.
Used in Bile Acid Homeostasis:
Fexaramine is used as a research compound to study the role of FXR in bile acid homeostasis. By acting as an FXR agonist, it can help protect cells and organs against bile acid toxicity and contribute to a better understanding of bile acid regulation mechanisms.
Used in Drug Development:
Fexaramine's selective and potent action on FXR makes it a valuable compound for drug development. It can be used as a lead compound or a reference for designing new drugs targeting FXR, which may have applications in treating various metabolic and inflammatory diseases.

Biological Activity

Potent, selective farnesoid X receptor agonist (EC 50 = 25 nM). Displays no activity at hRXR α , hPPAR α , hPPAR γ , hPPAR δ , mPXR, hPXR, hLXR α , hTR β , hRAR β , mCAR, mERR γ and hVDR receptors.

Biochem/physiol Actions

Fexaramine might regulate lipid and glucose metabolism and can serve as a therapeutic target in the treatment of fatty liver disease, type 2 diabetes and obesity. Fexaramine might mediate cholesterol homeostasis and promotes osteoblast differentiation and suppresses differentiation of osteoclast.

Upstream product

• 67-56-1 methanol 
• 28611-39-4 4-(dimethylamino)benzene-boronic acid 
• 1122-91-4 4-bromo-benzaldehyde 
• 2719-27-9 cyclohexanylcarbonyl chloride 
• 1041867-60-0 3-(3-tert-butoxycarbonylamino-phenyl)-acrylic acid 

Relevant academic research and scientific papers

NON-STEROIDAL FXR AGONISTS

ABSTRACT Potent non-steroidal farnesoid X receptor (FXR) agonists are N-aryl-N-arylmethyl amido and ureido compounds having the chemical structure represented by the following formula (I): INSERT FORMULA wherein E1 is (C1-C8)alkyl, cyclohexyl, 2-furyl, 3-

Discovery and optimization of non-steroidal FXR agonists from natural product-like libraries.

The efficient regulation of cholesterol biosynthesis, metabolism, acquisition, and transport is an essential component of lipid homeostasis. The farnesoid X receptor (FXR) is a transcriptional sensor for bile acids, the primary product of cholesterol metabolism. Accordingly, the development of potent, selective, small molecule agonists, partial agonists, and antagonists of FXR would be an important step in further deconvoluting FXR physiology. Herein, we describe the development of four novel classes of potent FXR activators originating from natural product-like libraries. Initial screening of a 10,000-membered, diversity-orientated library of benzopyran containing small molecules for FXR activation utilizing a cell-based reporter assay led to the identification of several lead compounds possessing low micromolar activity (EC50's = 5-10 microM). These compounds were systematically optimized employing parallel solution-phase synthesis and solid-phase synthesis to provide four classes of compounds that potently activate FXR. Two series of compounds, bearing stilbene or biaryl moieties, contain members that are the most potent FXR agonists reported to date in cell-based assays. These compounds may find future utility as chemical tools in studies aimed at further defining the physiological role of FXR and discovering potential therapeutic agents for the treatment of diseases linked to cholesterol and bile acid metabolism and homeostasis.