Fibrosis

Elexacaftor (VX-445) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. It promotes the processing and trafficking of CFTR, increases the amount of CFTR on the cell surface, and improves the processing and trafficking of Phe508del CFTR protein.

1. 3-Butylidenephthalide (Butylidene phthalide) has antihyperglycemic effect is due to inhibition of α-glucosidase at the intestinal level, inhibited the activity of yeast-α-glucosidase (IC(5) 2.35 mM) in a noncompetitive fashion with a K(i) of 4.86 mM.

Trimethylamine N-oxide dihydrate (TMANO Dihydrate), a product of the oxidation of trimethylamine, is considered as a protein stabilizer that may serve to counteract urea, the major osmolyte of sharks, skates and rays.

Deoxycorticosterone acetate (Cortexone acetate) is the 21-acetate derivative of desoxycorticosterone, used for intramuscular injection for replacement therapy of the adrenocortical steroid.

Derenofylline is a selective and potent adenosine A(1) antagonist in vitro (Ki=1 nM)

GLPG2938 (1-(2-Ethoxy-6-(trifluoromethyl)pyridin-4-yl)-3-((5-methyl-6-(1-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)pyridazin-3-yl)methyl)urea) is a potent and selective antagonist of S1P2.

TAK-615 is commonly used to study pulmonary fibrosis and is a negative allosteric modulator of LPA1 receptors.

Compound 6k, also known as Anti-hepatic fibrosis agent 2, is an orally active inhibitor of the COL1A1 enzyme and exerts anti-fibrogenic effects by targeting the Ewing sarcoma breakpoint region 1 (EWSR1)[1].

Gadopentetic acid (gadolinium complex) (Gd-DTPA) is an paramagnetic contrast agent commonly implemented by a bolus intravenous injection (i.v.) in Dynamic contrast-enhanced MRI (DCE-MRI) studies.

SEW 2871 is an orally available, highly selective S1P1 agonist with an EC50 of 13.8 nM.It reduces the number of lymphocytes in the blood and is used in studies related to diabetes, Alzheimer's disease, liver fibrosis, and inflammation. It activates ERK, Akt and Rac signaling pathways and induces S1P1 internalization and recycling.

Pirfenidone (AMR69) inhibits the production of CCL2 and CCL12 in fibroblasts and also decreases TGF-β2 protein levels. Pirfenidone is an antifibrotic agent that is commonly used in studies related to pulmonary fibrosis and also has anti-inflammatory activity.

Tauroursodeoxycholate (UR 906), also known as ursodoxicoltaurine, is a highly hydrophilic tertiary bile acid that is produced in humans at a low concentration. Tauroursodeoxycholate is the more hydrophilic form of ursodeoxycholic acid, which is the more abundant naturally produced bile acid in humans.Tauroursodeoxycholate is being investigated for use in several conditions such as Primary Biliary Cirrhosis (PBC), insulin resistance, amyloidosis, Cystic Fibrosis, Cholestasis, and Amyotrophic Lateral Sclerosis.

Trimethylamine N-oxide (TMAO) is a colorless amine oxide produced from choline, betaine, and carnitine via intestinal microbial metabolism that accumulates in tissues of marine animals and prevents the protein-damaging effects of urea.Trimethylamine N-oxide induces inflammation through activation of ROS NLRP3 inflammasomes, which can induce fibroblast differentiation and cardiac fibrosis.

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.

3-CPs (3-Carbethoxypsoralen) is a bleomycin-induced serotypic podoplanar polysaccharide in mouse lung fibrosis that belongs to the psoralen family and interferes with antibody-mediated bacterial killing.3-CPs delays bleomycin-induced lung fibrosis in mice and can be used in studies of airway inflammation and asthma.

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor (IC50: 15.3 nM) that reduces CCl4-induced hepatic fibrosis and exhibits anti-hepatic fibrosis effects.

Autotaxin-IN-4 is an Autotaxin inhibitor. It has the potential to treat idiopathic pulmonary fibrosis.

BPO-27 racemate (BPO-27 (racemate)) is an effective CFTR inhibitor with IC50 of 8 nM.

CFTR corrector 4 is a potent and orally available transmembrane conductance regulator (CFTR) for cystic fibrosis and is a potent (R,R) type active enantiomer. CFTR corrector 4 increases CFTR levels on the cell surface and is a potential compound for the study of cystic fibrosis.

DZ2002, an orally active, reversible, and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), exhibits significant immunosuppressive activity. It effectively prevents experimental dermal fibrosis by reversing the profibrotic phenotype in multiple cell types, making it useful for studying autoimmune diseases like lupus syndrome and systemic sclerosis.

GLPG1205 is a potent, orally active GPR84 (G protein-coupled receptor) antagonist with anti-inflammatory activity. GLPG1205 shows good PK PD characteristics and can be used to study pulmonary fibrosis.

Icosabutate (NST-4016) is an orally active derivative of eicosapentaenoic acid that inhibits hepatic inflammation and fibrosis in NASH, improves cardiovascular risk profiles in statin-treated patients with residual hypertriglyceridemia, lowers triglycerides, and may be useful in studies of liver fibrosis and atherosclerosis.

Tipelukast (KCA 757) is a novel, orally available leukotriene receptor antagonist with anti-inflammatory properties, capable of reducing fibrosis and down-regulating TIMP-1 and type 1 collagen. Tipelukast is utilized in asthma research.

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.