FXR Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S0037	Nidufexor (LMB-763)	Nidufexor (LMB763) is an agonist of farnesoid X receptor (FXR).
S8733	Tropifexor (LJN452)	Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. This compound shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR).
E4873	Mebhydroline	Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
S0874	Vonafexor (EYP001)	Vonafexor (EYP001, PLX007) is a novel non-bile acid, selective, second generation farnesoid X receptor (FXR) agonist.
S6547	Cilofexor (GS-9674)	Cilofexor(GS-9674) is a potent, selective oral agonist of farnesoid X receptor (FXR) with an EC50 of 43 nM. It has demonstrated anti-inflammatory, antifibrotic effects, and reduced portal pressure in preclinical liver fibrosis models, showing potential therapeutic benefit for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
E5874^New	INT-767	INT-767 is a dual agonist of farnesoid X receptor (FXR)/TGR5 with an EC50 of 0.033 μM and 0.67 μM, respectively. It significantly improves serum liver enzymes, hepatic inflammation, and biliary fibrosis, while inducing bile flow and biliary HCO₃⁻ output, making it a promising tool for chronic cholangiopathy research.
S0403	LY2562175	LY2562175 is a potent and selective agonist of FXR. This compound promotes transcriptional activation of human FXR in a cell-based cotransfection assay with EC50 of 193 nM.
E4617^New	Gly-β-MCA	Gly-β-MCA is a bile acid derivative that functions as a stable, orally active, and intestine-specific farnesoid X receptor (FXR) antagonist with potential therapeutic applications in metabolic diseases.
S7076	T0901317	T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of 20nM for LXRα and 5 μM for FXR, respectively. This compound is a dual inverse agonist of RORα and RORγ with Ki of 132 nM and 51 nM, respectively. It significantly suppresses cell proliferation and induces apoptosis.	J Clin Invest, 2025, 135(10)e186478 J Exp Med, 2025, 222(3)e20230647 Neurobiol Dis, 2025, 215:107094
S1643	Ursodiol	Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM)