SBI-115

SKU: orb1299827

Description

SBI-115 is a selective TGR5 antagonist used in research targeting polycystic liver disease. It has been shown to inhibit hepatic cystogenesis in preclinical models, making it a tool for studying TGR5 signaling in metabolic and liver disorders.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 882366-16-7
• MW: 340.78
• Purity: 99.78% (May vary between batches)
• Formula: C₁₄H₁₃ClN₂O₄S
• SMILES: CCS(=O)(=O)c1ncc(Cl)c(n1)C(=O)Oc1cccc(C)c1
• Target: GPCR19
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (11.74 mM);DMSO:150 mg/mL (440.17 mM)

Bioactivity

• In Vivo:
  Stimulation of cholangiocytes with TLCA following by SBI-115 treatment resulted in dose-dependent (by 32–48%) inhibition of cell proliferation.
• 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%.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

G protein-coupled Bile Acid Receptor 1, GPCR19, GPBAR1, G-protein coupled receptor 19, Inhibitor, inhibit, SBI 115, SBI115, SBI-115, TGR5

Compound Identifiers

PubChem CID

18879973