FXR Agonist

Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC₅₀ of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC₅₀ of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.

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

Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC₅₀ of 4 nM.

FXR agonist 3 is an anti-NASH agent, acting by activating FXR. FXR agonist 3 inhibits COL1A1, TGF-β1, α-SMA and TIMP1 expression with anti-fibrogenic activity. FXR agonist 3 significantly reduces liver steatosis and inflammation, improves liver fibrosis level.

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC₅₀s of 30 and 630 nM, respectively.

Isochenodeoxycholic acid (isoCDCA) is a FXR agonist. Isochenodeoxycholic acid activates the activity of FXR and induces the mRNA expression of FXR target genes (Ostβ and Kng1). Isochenodeoxycholic acid serves as a substrate for the liver class I ADH γγ isozyme-mediated 3β-dehydrogenation reaction.

Linafexor (CS-0159) is a FXR agonist and bile acid homeostasis modulator. Linafexor exerts its effects by activating FXR, a regulator of liver function. Linafexor is applicable to research related to primary sclerosing cholangitis (PSC). Linafexor is also suitable for research in the field of metabolic dysfunction-associated steatohepatitis (MASH).

Vonafexor (EYP001) is an orally active, non-steroidal and selective FXR agonist. Vonafexor shows significant HBsAg reduction when combined with Peg-IFNα. Vonafexor can be used for anti-HBV research.

EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC₅₀ values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.

Arjungenin, a pentacyclic triterpenoid compound, is a FXR agonist. Arjungenin can improve insulin sensitivity by regulating the function of fat cells. Arjungenin exhibits moderate free radical scavenging activity. Arjungenin has growth inhibitory activity against the insect Spilarctia obliqua. Arjungenin has significant antiviral activity against a series of viruses such as chikungunya Virus (CHIKV).

Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure.

Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).

Omesdafexor (MET409) is an orally active FXR agonist with a unique non-bile acid structure. Omesdafexor can be used for the study of non-alcoholic steatohepatitis (NASH).

PX20606 trans racemate (PX-102 trans racemate) is a FXR agonist with EC₅₀s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.

BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis.

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