||Obeticholic Acid (INT747; 6-ECDCA) is a novel derivative of cholic acid which acts as a potent and selective FXR agonist displaying anticholeretic activity in an in vivo rat model of cholestasis. It inhibits vascular smooth muscle cell inflammation and migration as well as promotes adipocyte differentiation and regulates adipose cell function in vivo.
||Fexaramine is an agonist of the farnesoid X receptor (FXR), which is a bile acid-activated nuclear receptor that controls bile-acid synthesis, conjugation and transport, as well as lipid metabolism through actions in the liver and intestine. Fexaramine has 100-fold greater affinity for FXR than natural compounds and described the genomic targets and binding site on FXR. When administered orally to mice, fexaramine produced selective actions through FXR receptors in the intestines.
||Levallorphan, also known as levallorphan tartate (USAN), is an opioid modulator of the morphinan family used as an opioid analgesic and opioid antagonist/antidote. It acts as an antagonist of the μ-opioid receptor (MOR) and as an agonist of the κ-opioid receptor (KOR), and as a result, blocks the effects of stronger agents with greater intrinsic activity such as morphine whilst simultaneously producing analgesia. As an agonist of the KOR, levallorphan can produce severe mental reactions at sufficient doses including hallucinations, dissociation, and other psychotomimetic effects, dysphoria, anxiety, confusion, dizziness, disorientation, derealization, feelings of drunkenness, and bizarre, unusual, or disturbing dreams. (Source: https://en.wikipedia.org/wiki/Levallorphan).
||Chenodiol, also known as Chenodeoxycholic Acid and chenocholic acid, is a bile acid. It occurs as a white crystalline substance insoluble in water but soluble in alcohol and acetic acid, with melting point at 165-167 °C. Salts of this carboxylic acid are called chenodeoxycholates. Chenodeoxycholic acid has been used as medical therapy to dissolve gallstones. Chenodeoxycholic acid can be used in the treatment of cerebrotendineous xanthomatosis. The Australian biotechnology company Giaconda has tested a treatment for Hepatitis C infection that combines chenodeoxycholic acid with bezafibrate.
||Turofexorate isopropyl, also known as WAY-362450 and XL335, is a highly potent, selective, and orally active agonist of the farnesoid X receptor (FXR) (EC(50) = 4 nM, Eff = 149%), which attenuates liver inflammation and fibrosis in murine model of non-alcoholic steatohepatitis
||GW4064是一种farnesoid X receptor (FXR)激动剂，CV1细胞系中EC50为65 nM。浓度达到1 μM时，对其他核受体没有活性。
||Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.