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Anti-NASH agent 2 (compound 21) is an inhibitor of neolipogenesis activity and α-SMA gene expression. It improves hepatic steatosis, edema, inflammatory infiltration, and liver fibrosis in NASH mouse models.

Anti-NASH Agent 1 (Compound 3d), derived from Elafibranor, serves as a strong PPAR-α δ agonist aimed at treating nonalcoholic steatohepatitis (NASH). At dosages of 3-10 mg kg over four weeks, this compound ameliorates hyperlipidemia, liver fat degeneration, and inflammation in a methionine-choline deficiency (MCD)-induced NASH mouse model, exhibiting minimal hepatotoxicity while providing substantial hepatic protection [1].

INT-767 is a potent farnesoid X receptor (FXR) TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

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.

Berberine ursodeoxycholate (HTD1801) is an orally effective hypolipidemic agent, an ionic salt of Berberine and Ursodeoxycholic acid.Berberine ursodeoxycholate has a wide range of metabolic activity and significantly reduces liver fat content. Berberine ursodeoxycholate has been used in studies of hyperlipidemia, non-alcoholic steatohepatitis (NASH) and diabetes.

Glycolithocholic acid (Lithocholic acid glycine conjugate) is a glycine conjugate of lithocholic acid.

Aramchol (C20-FABAC), also known as arachidyl amido cholanoic acid, is a conjugate of arachidic acid and cholic acid. It reduces ex vivo cholesterol crystallization in native human bile and dissolves pre-formed cholesterol crystals in a dose-dependent manner.

KHK-IN-5 (Compound 18), a KHK inhibitor, is employed in the study of nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and type 2 diabetes (T2DM).

HPG1860, an agonist of the farnesoid X receptor (FXR), induces luminescence in reporter gene assays utilizing HEK293T cells expressing human FXR, with an EC50 value of 18 nM. In vivo studies demonstrate that HPG1860 (administered at 1, 3, or 10 mg kg daily) reduces serum alanine aminotransferase (ALT) and total cholesterol levels in a mouse model of non-alcoholic steatohepatitis (NASH), which was induced by a high-fat diet and carbon tetrachloride (CCl4). Additionally, this compound decreases hepatic inflammation, fat levels, and fibrosis.

LH10 is an FXR agonist based on fexaramine, with an EC50 of 0.14 μM. It offers hepatoprotective effects, mitigating conditions such as cholestasis induced by alpha naphthylisothiocyanate (ANIT), acute liver injury caused by APAP, and non-alcoholic steatohepatitis (NASH).

FXR agonist12 (Compound C7) is an orally active FXR agonist. It downregulates bile acid synthesis-related genes and upregulates bile acid transport-related genes in HepG2 cells. FXR agonist12 alleviates ANIT-induced cholestasis and reduces liver damage and fibrosis in a mouse model of NASH.

DRX-065 is a stabilized and deuterated R-enantiomer of pioglitazone. DRX-065 has pharmacological properties desirable for the treatment of NASH (mitochondrial function modulation, non-steroidal anti-inflammatory effects, and glucose lowering effects) with

SHS4121705 is an orally bioavailable mitochondrial uncoupler.1It increases oxygen consumption rate in L6 rat myoblast cells with an EC50value of 4.3 μM. SHS4121705 (25 mg/kg per day in the diet) reduces hepatic steatosis, liver triglyceride levels, and plasma alanine aminotransferase (ALT) levels in Stelic animal model (STAM) mice, a model of non-alcoholic steatohepatitis (NASH). 1.Salamoun, J.M., Garcia, C.J., Hargett, S.R., et al.6-Amino[1,2,5]oxadiazolo[3,4-b]pyrazin-5-ol derivatives as efficacious mitochondrial uncouplers in STAM mouse model of nonalcoholic steatohepatitisJ. Med. Chem.63(11)6203-6224(2020)

MBX-8025 is an agonist of peroxisome proliferator-activated receptor δ (PPARδ).1 It is greater than 750- and 2,500-fold selective for PPARδ over PPARα and PPARγ. MBX-8025 (10 mg/kg per day for eight weeks) reduces increases in fasting blood glucose and serum insulin levels, and decreases insulin resistance in Alms1 mutant (foz/foz) mice fed an atherogenic diet as a model of diet-induced obesity, type 2 diabetes, and non-alcoholic steatohepatitis (NASH).2 It also decreases serum alanine transaminase (ALT), as well as serum and hepatic cholesterol and triglyceride, levels and reduces markers of NASH in the same model. |1. Bays, H.E., Schwartz, S., Littlejohn, T., 3rd, et al. MBX-8025, a novel peroxisome proliferator receptor-δ agonist: Lipid and other metabolic effects in dyslipidemic overweight patients treated with and without atorvastatin. J. Clin. Endocrinol. Metab. 96(9), 2889-2897 (2011).|2. Haczeyni, F., Wang, H., Barn, V., et al. The selective peroxisome proliferator-activated receptor-delta agonist seladelpar reverses nonalcoholic steatohepatitis pathology by abrogating lipotoxicity in diabetic obese mice. Hepatol. Commun. 1(7), 663-674 (2017).

ZLY032 is a dual agonist of free fatty acid receptor 1 (FFAR1/GPR40; EC50= 68 nM in a FLIPR assay) and peroxisome proliferator-activated receptor δ (PPARδ; EC50= 102 nM in a reporter assay).1It is selective for FFAR1 and PPARδ over PPARα and PPARγ (EC50s = >10 μM for both). ZLY032 (40 mg/kg, twice per day) reduces blood glucose levels in an oral glucose tolerance test and decreases plasma total cholesterol and triglyceride levels in theob/obmouse model of metabolic disease.2It reduces hepatic steatosis and plasma alanine transaminase (ALT) and aspartate aminotransferase (AST) levels in a mouse model of non-alcoholic steatohepatitis (NASH) induced by a methionine and choline-deficient diet at the same dose. 1.Li, Z., Chen, Y., Zhou, Z., et al.Discovery of first-in-class thiazole-based dual FFA1/PPARδ agonists as potential anti-diabetic agentsEur. J. Med. Chem.164352-365(2019) 2.Li, Z., Zhou, Z., Hu, L., et al.ZLY032, the first-in-class dual FFA1/PPARδ agonist, improves glucolipid metabolism and alleviates hepatic fibrosisPharmacol Res.159105035(2020)

Gardenoside has hepatoprotective, pain‑relieving, and anti-mastitis effects. it may be a potential therapeutic herb against NASH by suppressed supernatant inflammatory cytokine production and intracellular NFkB activity. Gardenoside may be considere

A3051, is a robust and orally active inhibitor of CXXC5-DVL with an IC 50 of 63.06 nM. Its applications include research into phenotypes associated with obesity, diabetes, and NASH that are induced by high fat diet (HFD) and methionine-choline deficient diet (MCD).

THR-β agonist 2 is a potent agonist of THR-β with potential for studies of metabolic diseases (e.g., obesity, hyperlipidaemia, hypercholesterolaemia, diabetes, steatosis, non-alcoholic steatohepatitis [NASH], atherosclerosis, and other related conditions).

THR-β agonist 4 is a potent THR-β agonist with significant research potential for treating metabolic diseases such as hyperlipidemia, obesity, hypercholesterolemia, diabetes, steatosis, non-alcoholic steatohepatitis (NASH), and atherosclerosis, as well as other related conditions.

THR-β agonist 3 is a potent agonist of THR-β with demonstrated research potential for metabolic diseases, including obesity, hyperlipidemia, hypercholesterolemia, diabetes, steatosis, non-alcoholic steatohepatitis (NASH), and atherosclerosis.

TRβ Agonist 1, a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, demonstrates an EC50 value of 21 nM. It is useful in the research of dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH) [1].

FXR antagonist 1 is a selective, orally active intestinal FXR antagonist with an IC50 value of 2.1 μM. FXR antagonist 1 antagonises intestinal FXR and selectively inhibits intestinal FXR signalling by feedback activation of hepatic FXR. FXR antagonist 1 can improve liver steatosis, inflammation and fibrosis in the NASH (non-alcoholic steatohepatitis) model and can be used to study NASH.

Glycolithocholic acid sodium salt, the sodium form of Glycolithocholic acid, is a glycine-conjugated secondary bile acid utilized in diagnosing ulcerative colitis (UC), non-alcoholic steatohepatitis (NASH), and primary sclerosing cholangitis (PSC).

Nivocasan, also known as GS-9450 and LB-84451, a novel caspase-inhibitor has demonstrated hepatoprotective activity in fibrosis apoptosis animal models. GS-9450 treatment induced significant reductions in ALT levels in NASH patients.