ipf

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

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.

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.

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

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.

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].

Flurbiprofen Axetil (Lipfen) is an anti-inflammatory used as an analgesic.

Progoitrin is a thioglucoside that is predominantly associated with infected crops. It has an inhibitory effect on thyroid activity.

8-iso Prostaglandin F2α ethanolamide (iPF2α-III ethanolamide; 8-Isoprostane ethanolamide; 8-iso PGF2α ethanolamide) is a derivative of isoprostane ethanolamide produced through the non-enzymatic free radical oxidation of arachidonoyl ethanolamide (AEA). It is commonly used as a biomarker for oxidative stress, helping to distinguish non-enzymatic breakdown products from enzyme-mediated prostamides generated via pathways such as COX-2.

2,3-Dinor-8-iso Prostaglandin F1α (2,3-dinor-8-iso PGF1α), an isoprostane and active metabolite of arachidonic acid deriving its formation from non-enzymatic free radical peroxidation, acts as an active metabolite of the platelet aggregation inhibitor 8-iso PGF2α. This compound exhibits vasoconstrictive properties in isolated porcine retinal and brain microvessels with EC50 values of 12.8 and 18.5 nM, respectively, yet it does not cause contraction in isolated rat aortic rings at a concentration of 31 µM. Further, at a concentration of 1 µM, it raises thromboxane B2 (TXB2) levels in isolated porcine brain slices, an effect reversible by thromboxane A synthase inhibitor CGS 12970, voltage-gated calcium channel inhibitor SKF 96365, or the nicotinic acetylcholine receptor (nAChR) antagonist α-conotoxin.

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 αVβ8 integrin inhibitor that suppresses the growth of multiple tumour cell lines (EMT6, CT26, KPC, TKCC-10). It may be employed in research concerning tumours, idiopathic pulmonary fibrosis (IPF), non-specific interstitial pneumonia (NSIP), and other conditions.

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).

TGF-β1/Smad3-IN-1 (Compound 5aa) is an orally administrable dual inhibitor of TGF-β1/Smad3 with anti-fibrotic activity and can be used for the study of idiopathic pulmonary fibrosis (IPF).