FXR Agonist

FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation.

HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC₅₀ of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC₅₀ values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH).

HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC₅₀ values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis.

Obeticholic Acid-d₄ is the deuterium labeled Obeticholic acid. 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.

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

FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.

Cholic acid 3-O-glucuronide (OCA-3-glucuronide) disodium is a farnesoid X receptor (FXR) agonist with an EC₅₀ value of 91.5 μM. Cholic acid 3-O-glucuronide is promising for research of bile acid metabolism and detoxification.

Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. 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.

BAR502 is a dual FXR and GPBAR1 agonist with IC₅₀ values of 2 μM and 0.4 μM, respectively.

LY2562175 is a potent and selective FXR agonist, with an EC₅₀ of 193 nM.

(R,R)-PX20606 is a FXR agonist with EC₅₀s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.

PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC₅₀ 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy.

BMS-986318 is a potent nonbile acid FXR agonist with EC₅₀s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis.

NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC₅₀ value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.

Obeticholic acid-d₅ is the deuterium labeled Obeticholic acid. 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.

Danifexor is the agonist for farnesoid X receptor.

FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models.

Alismanol M is a farnesoid X receptor (FXR) agonist with an EC₅₀ value of 50.25 μM. Alismanol M is a protostane-type triterpenoid that can be isolated from the rhizome of Alisma orientale. Alismanol M can be used for the research of cholestasis and nonalcoholic steatohepatitis.

FXR agonist 18 is an orally active FXR agonist, with an EC₅₀ of 10 nM against human FXR and an EC₅₀ of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.

LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC₅₀ of 51 nM measuring by TR-FRET assay, or an EC₅₀ of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis