IPF

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

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.

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

Dipfluzine is a diphenylpiperazine calcium channel blocker with poor solubility.

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.

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].

Bersiporocin is a novel prolyl-tRNA synthetase (PRS) inhibitor that exerts antifibrotic effects through downregulation of collagen synthesis and is well tolerated in the clinic. In cellular and animal models of idiopathic pulmonary fibrosis (IPF), DWN12088 significantly reduced collagen synthesis and improved lung function.

BAY-6672 is a selective human prostaglandin F (FP) receptor antagonist that is highly potent (IC50=11 nM), orally available and well permeable. It exerts antifibrotic effects by inhibiting prostaglandin F2α (PGF₂α) activity through antagonizing the FP receptor, and has in vivo efficacy in animal models of idiopathic pulmonary fibrosis (IPF).

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, a diarylhydrazone derivative, inhibits fibroblast activation and proliferation, positioning it as a candidate compound for the treatment of idiopathic pulmonary fibrosis (IPF).

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.

αVβ8-IN-1 is an inhibitor of the αVβ8 integrin. It exhibits growth-suppressive activity against tumors such as EMT6, CT26, KPC, and TKCC-10. αVβ8-IN-1 is suitable for research related to idiopathic pulmonary fibrosis (IPF), nonspecific interstitial pneumonia (NSIP), and various cancers.

GS-2278 is an antagonist of LPAR1 (lysophosphatidic acid receptor 1) with potential applications in the study of idiopathic pulmonary fibrosis (IPF).

HDAC6-IN-53 (Compound W28) is an inhibitor targeting histone deacetylase 6 (HDAC6) with an IC50 of 19.65 nM. It reduces the idiopathic pulmonary fibrosis (IPF) phenotype by inhibiting TGF-β1-induced collagen expression and demonstrates therapeutic efficacy in a bleomycin-induced mouse model of pulmonary fibrosis. HDAC6-IN-53 is applicable for research in idiopathic pulmonary fibrosis and related pulmonary fibrotic diseases.

S118 is an orally active inhibitor of the sphingosine-1-phosphate receptor 2 (S1P2 receptor). It prevents the binding of the S1P2 receptor to dapper1 (Dpr1), reduces the accumulation of β-catenin, and blocks the nuclear translocation of the S1P2 receptor. This process inhibits inflammation, fibrosis, and epithelial-mesenchymal transition (EMT), thereby exhibiting anti-idiopathic pulmonary fibrosis (IPF) activity. S118 is considered promising for research in idiopathic pulmonary fibrosis.

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.

(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor, exhibiting IC50 values of 61 nM for JNK1, 7 nM for JNK2, and 6 nM for JNK3. It selectively inhibits ERK1, p38α, and EGFR, with IC50 values of 0.48 μM, 3.4 μM, and 0.38 μM, respectively. In an acute rat PK-PD model, (3S)-Tanzisertib (hydrochloride) suppresses LPS-induced TNFα production and is utilized in research on idiopathic pulmonary fibrosis (IPF).

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.

Bexotegrast (PLN-74809) is an orally active and potent inhibitor of αvβ6 and αvβ1 integrins with antifibrotic effects, inhibiting αvβ6 and αvβ1-induced activation of TGF-β. It is applicable for studies of idiopathic pulmonary fibrosis (IPF) and non-specific interstitial pneumonia (NSIP).

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

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).

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).

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.

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).