FXR Inhibitors
| Cat.No. | Product Name | Information | Product Use Citations | Product Validations |
|---|---|---|---|---|
| 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. | ||
| E5874New | 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. | ||
| E4617New | 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. |
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| S1643 | Ursodiol | Ursodiol (Ursodeoxycholic acid, UDCA) reduces cholesterol absorption and is used to dissolve (cholesterol) gallstones. (IC50=0.22 μM) |
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