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SBI-115 is a TGR5 (GPCR19) antagonist, it decreases hepatic cystogenesis with polycystic liver diseases via inhibiting TGR5. SBI-115 inhibits proliferation triggered by pre-treatment of cystic cholangiocytes with Taurolithocholic acid (TLCA) in shRNA-transfected ADPKD cholangiocytes.
| Molecular Weight | 340.78 |
| Formula | C14H13ClN2O4S |
| CAS Number | 882366-16-7 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related GPCR19/TGR5 Products |
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| TGR5 Receptor Agonist
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist which showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5). |
| Deoxycholic acid sodium salt
Deoxycholic acid sodium salt is a bile acid and a by-product of intestinal metabolism, Deoxycholic acid sodium salt can activate the G protein-coupled bile acid receptor TGR5. |
| BAR 502
BAR502 is a dual agonist of FXR and GPBAR1 with IC50 values of 2 μM and 0.4 μM, respectively. |
| INT-777
INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM. In animal models, INT-777 alleviates liver injury by activating TGR5, thereby increasing bile flow and reducing bile acid synthesis. TGR5 signalling mediated by INT-777 induces the release of GLP-1 (glucagon-like peptide-1), improving liver and pancreatic function in obese mice. |
| SB756050
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment. |
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