Steatohepatitis is one type of liver disease which can be characterized by the inflammation and fat accumulation of liver which is a part of the alcoholic liver disease. It is otherwise called as fatty liver disease.
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MGL-3196 (VIA-3196, Resmetirom) is a potent and highly selective agonist of THR-β (Thyroid Hormone Receptor β) with EC50 of 0.21 uM; shows 28-fold selectivity for THR-β over THR-α in a functional assay; exhibits an excellent safety profile and orally bioactive.
Apararenone (MT-3995) is a novel potent, selective non-steroidal mineralocorticoid receptor antagonist for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
IVA-337 (Lanifibranor, IVA337)) is a potent, pan PPAR agonist with EC50 of 0.92 uM, 0.53 uM and 0.18 uM for human PPARα, PPARδ and PPARγ respectively; reduces skin fibrosis in the mouse, and suppresses inflammation in vivo.
Oltipraz (RP 35972, NSC 347901) is a cancer chemopreventive agent with inhibitory effect on angiogenesis and tumor growth, inhibits insulin- or hypoxia-induced HIF-1α expression through an increase in ubiquitination; abrogates insulin-induced H(2)O(2) production, thereby preventing H(2)O(2)-enhanced HIF-1alpha expression and promoting its ubiquitination and degradation; inhibits HIF-1α activity and HIF-1α-dependent tumor growth both in vitro and in vivo.
Tropifexor (LJN-452, LJN452) is a novel highly potent, selective, orally acitive FXR full agonist with EC50 of 0.26 nM; shows no significant off-target activity (>10,000-fold selectivity for FXR) in a panel of targets, including TGR5 (>10 uM); demonstratesin vivo activity in rodent PD models, and shows potential for treatment of cholestatic liver diseases and NASH.
Cilofexor (GS-9674, GS9674, PX-104) is a novel specific, non-steroidal farnesoid X receptor (FXR) agonist that reduces liver fibrosis and ameliorates portal hypertension in rat NASH models.
Emricasan (IDN-6556;PF-03491390) is a potent, irreversible pan-caspase inhibitor, shows neuroprotective activity for hNPCs, inhibits ZIKV-induced increased caspase-3 activity.
Selonsertib (GS-4997) is a highly selective and potent, ATP-competetive inhibitor of ASK1 (Apoptosis Signal-regulating Kinase 1, MAP3K5) with potential anti-inflammatory, antineoplastic and anti-fibrotic activities; orally bioavailable.
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