Formulation: A solid
Formal Name: (2R)-N-[2-[[3,3-dibutyl-2,3,4,5-tetrahydro-7-(methylthio)-1,1-dioxido-5-phenyl-1,5-benzothiazepin-8-yl]oxy]acetyl]-2-phenylglycyl-glycine
Purity: ≥98%
Formula Markup: C36H45N3O7S2
Formula Weight: 695,9
Shelf life (days): 1460
CAS Number: 439087-18-0
Notes: 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.
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