Fexaramine - CAS 574013-66-4
Catalog number: B0084-272107
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
Fexaramine is a small molecule farnesoid X receptor agonist with 100-fold increased affinity relative to natural compounds.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-272107 20 mg $298 In stock
Bulk Inquiry
Canonical SMILES:
1.3D-QSAR studies with the aid of molecular docking for a series of non-steroidal FXR agonists.
Zhang T;Zhou JH;Shi LW;Zhu RX;Chen MB Bioorg Med Chem Lett. 2007 Apr 15;17(8):2156-60. Epub 2007 Jan 31.
The farnesoid x receptor (FXR) has become a potential drug target for treating cholesterol-related and bile acid-related diseases recently. In this paper, 3-dimensional quantitative structure-activity (structure-affinity and structure-efficacy) relationships are investigated for a series of non-steroidal agonists (fexaramine series) by using the comparative molecular field analysis (CoMFA), where molecular docking method (FlexX) is employed to construct molecular superimposition maps. A proposal to design some new agonists is discussed lastly.
2.Farnesoid X receptor agonist decreases lipid accumulation by promoting hepatic fatty acid oxidation in db/db mice.
Liu Y;Song A;Yang X;Zhen Y;Chen W;Yang L;Wang C;Ma H Int J Mol Med. 2018 Sep;42(3):1723-1731. doi: 10.3892/ijmm.2018.3715. Epub 2018 Jun 5.
The development of type‑2 diabetes and its complications is associated with lipid metabolism disorder. Farnesoid X receptor (FXR) has an important role in regulating lipid and glucose metabolism. However, the underlying mechanism of this remains unclear. The present study investigated the role of fexaramine (Fex), an FXR agonist, on lipid metabolism. For this purpose, 6‑week‑old db/db mice were treated with Fex for 8 weeks via oral gavage and db/db mice treated with corn oil were used as controls. Body weight and food intake were monitored daily and bi‑weekly, respectively. A glucose tolerance test was performed during the final week of feeding. Blood samples were obtained for the analysis of lipids and enzymes related to hepatic function, and liver tissues were analyzed by histology and molecular examination. The results indicated that serum and liver triglyceride levels were decreased in db/db mice administered with Fex. Fewer small lipid droplets were observed in the liver. Small heterodimer partner (SHP), a downstream gene of FXR, was upregulated following Fex treatment. The mRNA and protein expression of genes associated with fatty acid oxidation [acetyl coenzyme A carboxylase (ACC), carnitine palmitoyl transferase 1α (CPT1‑α) and peroxisome proliferator‑activated receptor‑coactivator‑1α] was also increased.
3.Intestine farnesoid X receptor agonist and the gut microbiota activate G-protein bile acid receptor-1 signaling to improve metabolism.
Pathak P;Xie C;Nichols RG;Ferrell JM;Boehme S;Krausz KW;Patterson AD;Gonzalez FJ;Chiang JYL Hepatology. 2018 Feb 27. doi: 10.1002/hep.29857. [Epub ahead of print]
Bile acids activate farnesoid X receptor (FXR) and G protein-coupled bile acid receptor-1 (aka Takeda G protein-coupled receptor-5 [TGR5]) to regulate bile acid metabolism and glucose and insulin sensitivity. FXR and TGR5 are coexpressed in the enteroendocrine L cells, but their roles in integrated regulation of metabolism are not completely understood. We reported recently that activation of FXR induces TGR5 to stimulate glucagon-like peptide-1 (GLP-1) secretion to improve insulin sensitivity and hepatic metabolism. In this study, we used the intestine-restricted FXR agonist fexaramine (FEX) to study the effect of activation of intestinal FXR on the gut microbiome, bile acid metabolism, and FXR and TGR5 signaling. The current study revealed that FEX markedly increased taurolithocholic acid, increased secretion of fibroblast growth factors 15 and 21 and GLP-1, improved insulin and glucose tolerance, and promoted white adipose tissue browning in mice. Analysis of 16S ribosomal RNA sequences of the gut microbiome identified the FEX-induced and lithocholic acid-producing bacteria Acetatifactor and Bacteroides. Antibiotic treatment completely reversed the FEX-induced metabolic phenotypes and inhibited taurolithocholic acid synthesis, adipose tissue browning, and liver bile acid synthesis gene expression but further increased intestinal FXR target gene expression.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related FXR Products

(CAS: 1103500-20-4)

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


EP-024297 is a novel agonist of farnesoid X receptor (FXR). Study in Chinese hamster ovary cells showed that it is 20000-fold more potent than obeticholic acid ...

CAS 278779-30-9 GW4064

(CAS: 278779-30-9)

GW4064 is a selective non-steroidal agonist of farnesoid X receptor (FXR) with EC50 value of 15 nM.

CAS 1000403-03-1 INT-767

(CAS: 1000403-03-1)

INT-767, a steride compound, has been found to be a inhibitor of FXR and TGF5 and could have probable effect against some liver and metabolic diseases. It was j...

CAS 1612191-86-2 BAR502

(CAS: 1612191-86-2)

BAR502 is a dual FXR and GPBAR1 agonist (IC50= 2 μM and 0.4 μM for FXR and GPBAR1, respectively).

CAS 1383816-29-2 Tropifexor

(CAS: 1383816-29-2)

Tropifexor is a novel highly potent agonist of farnesoid X receptor (FXR), which regulates bile acid metabolism and signaling. FXR activated by Tropifexor can i...

CAS 474-25-9 Chenodeoxycholic Acid

Chenodeoxycholic Acid
(CAS: 474-25-9)

Chenodeoxycholic Acid is a naturally occurring human bile acid.Chenodeoxycholic acid has been used as medical therapy to dissolve gallstones.

CAS 459789-99-2 Obeticholic Acid

Obeticholic Acid
(CAS: 459789-99-2)

Obeticholic Acid is a potent and selective farnesoid X receptor (FXR) agonist with EC50 of 99 nM. It reduced liver fat and reverted cholestasis in a rat model.

(CAS: 1609564-75-1)

DY-268, a pyrazol carboamide derivative, has been found to be a FXR antagonist that could be significant in studies of the biological activities of FXR. IC50: 7...

PX 102
(CAS: 1268245-19-7)

PX102 is a Farnesoid X-activated Receptor (FXR) agonist originated by Phenex Pharmaceuticals. PX102 demonstrated potent plasma cholesterol-lowering activity tha...

CAS 629664-81-9 Turofexorate Isopropyl

Turofexorate Isopropyl
(CAS: 629664-81-9)

Turofexorate Isopropyl is a highly potent, selective, and orally active farnesoid X receptor (FXR) agonist.

(CAS: 1268244-85-4)

PX-102, also known as PX-20606, is a farnesoid X-activated receptor (FXR) agonist. PX-102 is indicated to be active in lowering plasma cholesterol, and ameliora...

CAS 574013-66-4 Fexaramine

(CAS: 574013-66-4)

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

CAS 39025-23-5 Z-Guggulsterone

(CAS: 39025-23-5)

Z-Guggulsterone is a broad spectrum steroid receptor ligand that acts as a mineralocorticoid, progesterone and glucocorticoid receptor antagonist (Ki = 37, 224 ...

CAS 1198085-23-2 PX 20350

PX 20350
(CAS: 1198085-23-2)

PX 20350 is a farnesoid X receptor (FXR) agonist with enhanced affinity and efficacy (12 nM and 109% (compared to GW 4064)) in FXR FRET assay and full length FX...

Chemical Structure

CAS 574013-66-4 Fexaramine

Quick Inquiry

Verification code

Featured Items