ipf

Isoprostanes are prostaglandin (PG)-like products of free-radical induced lipid peroxidation. Although the isoprostanes derived from arachidonic acid are the best characterized, many other polyunsaturated fatty acids can form isoprostanes. (±)5-iPF2α-VI is one of dozens of possible stereo- and regioisomeric isoprostanes which can be formed from arachidonic acid. To date, the most extensively studied of these is 8-isoprostane (8-epi-PGF2α, iPF2α-III). However, 8-isoprostane is a minor isoprostane constituent when compared to some of the other isomers which form in natural conditions of oxidative stress. (±)5-iPF2α-VI is an isoprostane from the unique Type VI class of isoprostanes. This class has been shown to be one of the major isoprostane products, in contrast to 8-isoprostane. In addition to being produced in greater abundance than 8-isoprostane, Type VI isoprostanes form internal lactones, which facilitates their extraction and purification from biological samples.

8,12-iso-iPF2α-VI, an isoprostane, arises from non-enzymatic, free radical-induced peroxidation of membrane lipids. It is the predominant isoprostane formed during lipid peroxidation and serves as a biomarker for oxidative stress. Detectable in hepatic tissue post CCl4-induced oxidative damage, 8,12-iso-iPF2α-VI levels are also elevated in the urine, blood, and cerebrospinal fluid of Alzheimer’s disease patients.

TGFβ1-IN-2, a derivative of diarylacylhydrazones, effectively inhibits fibroblast activation and proliferation and holds potential for idiopathic pulmonary fibrosis (IPF) research [1].

TGFβ1-IN-3 is a diarylhydrazone derivative with inhibitory effects on fibroblast activation and proliferation.TGFβ1-IN-3 is a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF).

Ipfencarbazone herbicide agent, is a substance being developed for the control of weeds such as watergrass in rice.

Ipflufenoquin, an insecticide, effectively combats primary apple scab infections. Its application is optimal between the stages of half an inch of green and fruit set [1].

Dipfluzine is a diphenylpiperazine calcium channel blocker with poor solubility.

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibits αvβ6 and αvβ1-induced activation of TGF-β, and can be used for the study of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

Macitentan n-butyl analogue, a derivative of Macitentan, functions as an orally active dual antagonist targeting both endothelin ETA and ETB receptors. This compound shows promise for treating idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH), leveraging its non-peptide structure for potential therapeutic applications.

ATX inhibitor 12 is an orally active ATX inhibitor (IC50: 1.72 nM). In C57Bl/6J mice, oral administration of ATX inhibitor 12 at a dose of 60 mg/kg was effective in inhibiting structural lung damage and reducing fibrotic lesions.

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

TP0556351, a potent and selective inhibitor of matrix metalloproteinase-2 (MMP2), exhibits significant efficacy with an IC50 of 0.2 nM and demonstrates the capability to decrease collagen accumulation in a Bleomycin-induced pulmonary fibrosis mouse model. This compound shows promise as a research tool for idiopathic pulmonary fibrosis (IPF) [1].

BMS-986020 (AM152) is a selective antagonist of LPA1.

Pamrevlumab (FG-3019) is a human antibody with affinity for connective tissue growth factor (CTGF) and is involved in anti-CTGF therapy for the treatment of idiopathic pulmonary fibrosis (IPF).

Andecaliximab is a recombinant IgG4 monoclonal antibody targeting matrix metalloproteinase 9 (MMP9). Andecaliximab showed antifibrotic effects in a mouse model of idiopathic pulmonary fibrosis. Andecaliximab can be used to study gastric adenocarcinoma and idiopathic pulmonary fibrosis (IPF), as well as dengue virus.

PDE1-IN-4 is a potent and selective inhibitor of PDE1 (phosphodiesterase-1), acting on PDE1C (IC50: 10 nM), PDE1A (IC50: 145 nM) and PDE1B (IC50: 354 nM). PDE1-IN-4 regulates cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate) and exhibits antifibrotic effects. PDE1-IN-4 can inhibit TGF-β1-induced differentiation of human lung fibroblasts, and can be used to study idiopathic pulmonary fibrosis (IPF).

PI3K/mTOR Inhibitor-13, an orally active dual inhibitor targeting phosphoinositol 3-kinase (PI3K) and mTOR kinase, holds potential for treating sexual diseases, solid tumors, and idiopathic pulmonary fibrosis (IPF).

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.

Corilagin has anti-inflammatory activity. Corilagin has a significant antitumour potential and lower toxicity in normal cells in vitro.Corilagin can enhance the cytotoxicity of both cisplatin and doxorubicin on the Hep3B hepatoma cells.Corilagin has antiviral activity, reduces the cytotoxicity induced by EV71 or CA16 on Vero cells with and IC50 value of 5.6 and 32.33 μg/mL, respectively. Corilagin shows the potential to protect against HSV-1-induced encephalitis, and the beneficial effects may be mediated by inhibiting TLR2 signaling pathways.Corilagin has antifibrotics property and is potentiated in treating idiopathic pulmonary fibrosis(IPF), attenuates bleomycin-induced epithelial injury and fibrosis via inactivation of oxidative stress, proinflammatory cytokine release and NF-κB and TGF-β1 signaling. Solvent:Pyridine, Methanol, Ethanol, etc.

CC-90001 is an orally administered c-Jun N-terminal kinase (JNK) inhibitor with bias for JNK1 over JNK2.

Ifabotuzumab (KB004), an IgG1κ antibody, specifically binds to EphA3 (K D =610 pM), inducing tumor cell apoptosis, activating antibody-dependent cell-mediated cytotoxicity (ADCC), and damaging tumor vasculature. Additionally, Ifabotuzumab effectively reduces CCR10+ cells in human idiopathic pulmonary fibrosis (IPF) and ameliorates pulmonary fibrosis, demonstrating its therapeutic potential [1] [2].

Thi-DPPY is a potent, orally active JAK3 inhibitor that acts on BTK (IC50: 62.4 nM), JAK (IC50: 1.38 nM). Thi-DPPY is anti-proliferative against HBE cells. Thi-DPPY has anti-inflammatory effects in vivo. Thi-DPPY has shown research potential in idiopathic pulmonary fibrosis (IPF).

BMS-986020 sodium is a high-affinity lysophosphatidic acid receptor 1 (LPA1) antagonist that inhibits bile acids and phospholipid transport proteins, and inhibits BSEP (IC50: 4.8 μM), MRP4 (IC50: 6.2 μM) and MDR3 (IC50: 7.5 μM). BMS-986020 sodium showed potential for the study of idiopathic pulmonary fibrosis (IPF).

STAT3-IN-15, a potent and orally active inhibitor targeting STAT3, effectively combats idiopathic pulmonary fibrosis (IPF) by hindering STAT3 phosphorylation. Additionally, it impedes TGF-β1-induced migration and deformation of epithelial cells and prevents epithelial-mesenchymal transition (EMT), offering a multifaceted approach against IPF.

FAP-PI3KI1, a fibroblast-activated protein (FAP)-targeted PI3K inhibitor, selectively targets FAP-expressing human idiopathic pulmonary fibrosis (IPF) cells. It effectively inhibits collagen synthesis and reduces collagen deposition [1].

DPPY is a potent inhibitor of PTK that acts on EGFR (IC50<10 nM), BTK (IC50<10 nM), and JAK3 (IC50<10 nM). DPPY inhibits the proliferation of B-cell lymphoma cells and has potential for investigation in idiopathic pulmonary fibrosis (IPF).