| Name | SBI-115 |
| Description | SBI-115 is an antagonist of TGR5. SBI-115 decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5 |
| Cell Research | 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%. |
| In vivo | Stimulation of cholangiocytes with TLCA following by SBI-115 treatment resulted in dose-dependent (by 32–48%) inhibition of cell proliferation. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 150 mg/mL (440.17 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (11.74 mM), Sonication is recommended.
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| Keywords | TGR5 | SBI-115 | SBI115 | SBI 115 | Inhibitor | inhibit | G-protein coupled receptor 19 | GPCR19 | GPBAR1 | G protein-coupled Bile Acid Receptor 1 |
| Inhibitors Related | Taurodeoxycholic acid | Ursodeoxycholic acid sodium | BAR502 | TC-G 1005 | Triamterene | Deoxycholic acid | L-692429 | Ursodeoxycholic acid | Deoxycholic acid sodium salt | Sodium taurodeoxycholate hydrate | Hyodeoxycholic acid | PEN (human) aceate |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Multi-Target Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
