SBI-115 是TGR5 (GPCR19)拮抗剂，对 TGR5 降低多囊性肝病的肝囊肿形成具有抑制作用。

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

Stimulation of cholangiocytes with TLCA following by SBI-115 treatment resulted in dose-dependent (by 32–48%) inhibition of cell proliferation.

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%.

882366-16-7

C14H13ClN2O4S

340.78

DMSO:150 mg/mL (440.17 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years