cholangitis

Glycolithocholic acid (Lithocholic acid glycine conjugate) is a glycine conjugate of lithocholic acid.

Linerixibat (GSK2330672) is a highly effective, nonabsorbable ASBT inhibitor (IC50: 42 ± 3 nM) that can lower glucose in an animal model of type 2 diabetes and demonstrates excellent developability properties.

24-Norursodeoxycholic acid (nor-UDCA) is a side chain-shortened C23 homolog of UDCA.It has shown potent anti-inflammatory, anti-cholestatic, and anti-fibrotic properties.It is a Ursodeoxycholic Acid derivative. It is superior to Ursodeoxycholic acid in the treatment of sclerosing cholangitis in Mdr2 (Abcb4) knockout mice

NHS-activated 2-octynoic acid-BSA is an immunogen utilized to develop a mouse model for primary biliary cholangitis (PBC). When combined with Complete Freund's Adjuvant, it stimulates the immune system to recognize it as a foreign antigen, triggering an immune response against the body's biliary epithelial cells. This results in the production of anti-PDC-E2 antibodies, causing bile duct damage and inflammation. NHS-activated 2-octynoic acid-BSA is promising for primary biliary cholangitis research.

Linafexor (CS-0159) is a non-steroidal FXR (farnesoid X receptor) agonist for studying primary sclerosing cholangitis (PSC) and non-alcoholic steatohepatitis (NASH).

Elafibranor (GFT505) sulfoxide is a sulfoxide metabolite of Elafibranor, which acts as an agonist for PPARα/δ with EC50 values of 45 nM and 175 nM, respectively. Elafibranor is utilized in research related to primary biliary cholangitis.

INVA8001 is a highly selective and orally active chymase inhibitor, with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell protease 4 (mMCP-4). It exhibits IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, demonstrating over 1000-fold selectivity against other related serine proteases. In a mouse model of primary sclerosing cholangitis (PSC), INVA8001 inhibits mast cell activity, improves biliary pathology, alleviates cholestasis, and displays anti-inflammatory and anti-fibrotic properties.

Glycolithocholic acid sodium salt, the sodium form of Glycolithocholic acid, is a glycine-conjugated secondary bile acid utilized in diagnosing ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH), and primary sclerosing cholangitis (PSC).

Meloxicillin is a broad-spectrum penicillin antibiotic that is active against both Gram-negative bacteria and some Gram-positive bacteria. Unlike most other broad-spectrum penicillin, it is excreted by the liver and can therefore be used to treat biliary

Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 / αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activation of TGF-β1 in actively fibrotic tissue. Inhibition of these integrins will block TGF-β1 activation, thereby preventing the growth of fibrotic tissue within the lung and bile ducts.

BMS-986339 is an orally active, potent FXR agonist that engages His298 and ASN287 residues via H-bond formation. It is employed in research on primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH) due to its anti-fibrosis properties.

EDP-305 is an orally active, potent, and highly selective non-bile acid farnesoid X receptor (FXR) agonist with EC₅₀ values of 34 nM (chimeric FXR) and 8 nM (full-length FXR). By activating FXR, EDP-305 modulates pathways related to bile acid, lipid, and glucose metabolism and inhibits inflammation and fibrosis-related signaling; consequently, it is used in research on liver diseases such as non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis, and liver fibrosis. EDP-305 reduces levels of liver lipid accumulation, inflammation, and fibrosis markers while improving liver function parameters, and is regarded as a promising FXR-targeted metabolic modulator.

Simtuzumab is a monoclonal antibody against lysyl oxidase-like protein 2 (LOXL2). Simtuzumab can be used to treat primary sclerosing cholangitis (PSC) and is not effective in patients with bridging fibrosis or compensatory cirrhosis caused by non-alcoholic steatohepatitis.

Timolumab (BTT 1023), a fully human antibody targeting vascular adhesion protein-1 (VAP-1), attenuates fibrosis in a mouse model of liver injury and may be used to study primary sclerosing cholangitis.

FFP-104 is a humanized IgG4 monoclonal antibody inhibitor that targets TNFRSF5/CD40. VX70 is applicable for research into chronic autoimmune liver diseases, such as primary biliary cholangitis (PBC).

Anti-Mouse CD40L/CD154 Antibody (MR-1) is a monoclonal inhibitory antibody targeting mouse CD40L/CD154. It downregulates the expression of the IFN signaling pathway and reduces IFN-β production, effectively prolonging graft survival. It can be used in research on cancer, inflammatory diseases, and xenotransplantation, including pancreatic cancer and autoimmune cholangitis.