fxr

FXR/TGR5 agonist 1 acts as an agonist on both FXR and TGR5 receptors and is utilized for treating fatty liver disease.

Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.

INT-767 is a potent farnesoid X receptor (FXR)/TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,

Altenusin is a natural nonsteroidal fungal metabolite, as a novel selective agonist of FXR with an EC50 value of 3.2 ± 0.2 μM.

Chenodeoxycholic acid (CDCA) is a bile acid that inhibits 11β-HSD2 with an IC50 value of 22 mM. Chenodeoxycholic acid acts as a detergent to dissolve fat for intestinal absorption and is reabsorbed by the small intestine. Chenodeoxycholic acid is used as a choledocholithiasis, choledocholithiasis and laxative, as well as to prevent or dissolve gallstones.

Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a toxic secondary bile acid, They were FXR antagonists (IC50=0.7, 1.4 μM), EphA2 antagonists (IC50=48, 66 μM) and EphB4 antagonists (IC50=141 μM). Lithocholic acid can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is a cleanser that dissolves fat for absorption and is itself absorbed.

Sevelamer hydrochloride (Sevelamer HCl) is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.

Chenodeoxycholic Acid sodium salt (CDCA sodium salt) is a bile acid in humans that activates the nuclear receptor FXR, rescues axonal degeneration of induced pluripotent stem cell-derived neurons in patients with spastic paraplegia type 5 and cerebral xanthomatosis, and can be used to study pancreatic necrosis.

BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).

Gly-β-MCA is an orally bioactive, enteroselective and potent inhibitor of the farnesoid X receptor (FXR), a bile acid, used in the study of obesity and diabetes.

Glyco-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an agonist of the farnesoid X receptor (FXR).

Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).

Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).

LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).

GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).

Vidofludimus (SC12267) (4SC-101, SC12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (DHODH).

Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.

Androsterone, a metabolic product of testosterone, can activate Farnesoid X Receptor (FXR).

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM

NDB is a selective and potent hFXRα antagonist that inhibits GW4064-stimulated FXR/RXR interactions and FXRα target gene expression in primary mouse hepatocytes.NDB is used in the study of diabetes.

T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).

Osocimab (BAY 1213790) is a potent anti-FXIa antibody with a Ki value of 2.4 nM and an EC50 value of 0.2 nM.Osocimab may reduce thrombosis through FXI inhibition.Osocimab is often used as an XI factor inhibitor, has an inhibitory effect on thrombin generation, has an anticoagulant effect, and is used in the study of thromboembolic diseases. Thromboembolic Diseases