anti-fibrotic

Taxifolin (Dihydroquercetin) is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

Ro24-7429 is a small molecule inhibitor, an HIV-1 Tat antagonist and RUNX1 inhibitor, with oral activity, cell permeability, and anti-inflammatory effects, used for anti-HIV, anti-fibrotic, and inflammation-related research.

Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.

OATD-01 is a highly active inhibitor of both Chitotriosidase (CHIT1) and acidic mammalian chitinase (AMCase).

Antifibrotic agent 1 is an orally active medication designed to treat idiopathic pulmonary fibrosis (IPF). It effectively mitigates IPF-related processes, including TGF-β-induced epithelial-mesenchymal transition (EMT) and fibroblast-to-myofibroblast transition (FMT), as well as profibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α, and Src family kinases (SFKs), while sparing VEGFR, FGFR, and Abl to minimize off-target toxicity. In a bleomycin (BLM)-induced pulmonary fibrosis mouse model, it demonstrates strong antifibrotic activity.

Malotilate (Kantec) is a medicine used for the therapy of liver cirrhosis.

Aucubin (Rhinanthin) is an iridoid glycoside with anti-inflammatory, anti-microbial, anti-algesic as well as anti-tumor activities.

Belumosudil (Rezurock) is an orally available, and specific ROCK2 inhibitor (IC50/Ki: 60/41 nM).

SC-43 is a potent and orally active agonist of SHP-1 (PTPN6). SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis, and with anti-fibrotic and anticancer effects.

TD139 is a small molecule inhibitor of inhaled galectin-3 (Gal-3) with potential anti-fibrotic activity, commonly used in the study of idiopathic pulmonary fibrosis.

Saracatinib (AZD0530) is a small molecule inhibitor belonging to the Src family kinase inhibitors (IC50=2.7–11 nM), featuring high selectivity, cell permeability, and oral bioavailability, with anti-fibrotic, anti-inflammatory, and potential anti-tumor activities.

Selvigaltin (GB1211) is an orally administered, highly selective small-molecule inhibitor of galectin-3 (Gal-3) with an IC₅₀ value of 12 nM in rabbits, exhibiting anticancer and anti-fibrotic activity. Selvigaltin reduces galectin-3 levels in the liver and decreases biomarkers of inflammation (cellular foci) and fibrosis (PSR, SHG), while simultaneously lowering the mRNA and protein expression of inflammatory and fibrotic biomarkers (IL-6, TGF-β3, SNAI2, collagen). Selvigaltin also restores T-cell activity and reduces tumor growth and metastasis. Selvigaltin is suitable for use in studies of liver fibrosis, non-alcoholic steatohepatitis (NASH), and tumors.

Fezagepras sodium (Setogepram sodium salt) is an orally active GPR40 agonist and is an antagonist or inverse agonist for GPR84, with anti-fibrotic, anti-inflammatory and anti-proliferative actions.

Idoxifene (CB7432) is a selective and tissue-specific estrogen receptor modulator (SERM) that reduces collagen and malondialdehyde (MDA) levels in rat liver, exhibiting anti-fibrotic effects.

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

Cenicriviroc Mesylate is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2 with anti-inflammatory and antiinfective activity.

PXS-5120A is an irreversible fluoroallylamine Lysyl Oxidase-like 2/3 (LOXL2/3) inhibitor with anti-fibrotic activity.

Fezagepras (Setogepram) is an orally active GPR40 agonist and is an antagonist or inverse agonist of GPR84 with anti-inflammatory, anti-fibrotic, and anti-proliferative actions.

Chiglitazar is a PPAR α/γ/δ agonist and insulin sensitizer used in the treatment of type 2 diabetes mellitus to lower blood glucose, regulate blood lipids, and have anti-inflammatory and anti-fibrotic effects.

KIRA-7 is an imidazopyrazine compound. KIRA-7 has an anti-fibrotic effect. KIRA-7 binds the IRE1α kinase (IC50: 110 nM) to allosterically inhibit its RNase activity.

ML-290 is an effective relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes. It shows an EC50 of 94 nM.

BPU17 interacts with PHB1 and disrupts the PHB1-PHB2 interaction, causing slight mitochondrial dysfunction. This damage hinders transcription dependent on SRF/CArG-box, thereby inhibiting epithelial-mesenchymal transition (EMT) in retinal pigment epithelial cells (RPEs). BPU17 has demonstrated anti-fibrotic activity in vivo. It holds potential as a research agent for anti-angiogenic age-related macular degeneration (nAMD).

RIPK2-IN-6 (Compound 15a) is an inhibitor of RIPK that specifically targets the phosphorylation of RIPK2, thereby suppressing the NF-κB and MAPK signaling pathways. It has demonstrated anti-inflammatory and anti-fibrotic activities in a mouse model of colitis induced by Dextran sodium sulfate.

LOX-IN-5 tosylate (compound 22) is a selective oral inhibitor of lysyl oxidase-like 2 (LOXL2) with an IC50 of less than 300 nM, and it exhibits anti-fibrotic properties.