FXR antagonist 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.

(E)-Guggulsterone is an isomer of guggulsterone. As an FXR antagonist, it reduces blood lipids, induces heme oxygenase-1 expression, blocks DENV NS2B/3B activity, and inhibits DENV replication.

Compound A-26, also known as FXR antagonist 2, is a diarylamide derivative that functions as a moderate FXR antagonist. It is utilized in researching hyperlipidemia and type 2 diabetes [1].

Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, serves as a competitive and reversible FXR antagonist (IC50 = 40 μM) and demonstrates antiapoptotic effects by preventing bile acid-induced hepatocellular apoptosis and maintaining mitochondrial membrane potential [1][2].

F44-A13 is an orally active, highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. It optimizes cholesterol metabolism and reduces activity by inducing CYP7A1 expression, lowering cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) levels in mouse models. F44-A13 is applicable for studying metabolic diseases associated with lipid disorders [1].

(E)-Guggulsterone (Standard) is a reference standard for research and analysis in studies involving (E)-Guggulsterone. (E)-Guggulsterone is an isomer of guggulsterone. As an FXR antagonist, it reduces blood lipids, induces heme oxygenase-1 expression, blocks DENV NS2B/3B activity, and inhibits DENV replication.