SBI-115 is an antagonist of TGR5. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5

cAMP was detected by the Bridge-It cAMP designer cAMP assay. Cholangiocytes (10,000/well) were incubated with TLCA, OA, C1 and C2 (all, 25 μM), SBI-115 (100 and 200 μM) and pasireotide (20 μM) for 15–30 min. Doses of drugs were chosen based on published data or dose ranging (SBI-115). Cell proliferation was determined by CellTiter 96 Aqueous One Solution Cell Proliferation Assay ?and by cell counting using the Cellometer Auto4 ?cell counter.?Cholangiocytes (2500 cells/well) were grown for 24–48 hours and then treated with TGR5 agonists (all, 25 μM), SBI-115 (100 and 200 μM) and pasireotide (20 μM) for additional 24 hours.?Alterations in cell proliferation after treatment were expressed as percent change compared to un-treated cholangiocytes in which cell proliferation was considered to be equal 100%.