产品描述:
Elobixibat is an inhibitor of the sodium/bile acid and sulfated solute cotransporter (ASBT), also known as the ileal bile acid transporter (IBAT; IC50s = 0.53, 0.13, and 5.8 nM for the human, mouse, and canine transporters, respectively).{66752} It is selective for ASBT over the hepatic sodium/bile acid cotransporter (IC50 = 240 nM). Elobixibat induces mild giant migrating contractions in the colon and increases the number of defecations in conscious dogs two hours after administration of 3, 10, or 30 mg/kg doses, as well as increases the number of defecations after ten hours at 30 mg/kg.{66753} Oral administration of elobixibat (1.2 mg/kg per day) reduces methionine- and choline-deficient diet-induced increases in serum bile acid levels and hepatic inflammation, fibrosis, and cytokine gene expression in a mouse model of non-alcoholic steatohepatitis (NASH).{66754} Formulations containing elobixibat have been used in the treatment of chronic constipation.