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.
|Solubility (25°C)||DMSO ≥ 90 mg/mL|
Powder -20°C 3 years ; 4°C 2 years
In solvent -80°C 6 months ; -20°C 1 month
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Related GPCR19/TGR5 Products|
|Ursodeoxycholic acid sodium
Ursodeoxycholic acid (Ursodeoxycholate) sodium is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism.
SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.
|Deoxycholic acid sodium salt
Deoxycholic acid sodium salt activates the G protein-coupled bile acid receptor TGR5.
INT-777 is a potent TGR5 agonist with EC50 of 0.82 μM.
BAR502 is a dual agonist of FXR and GPBAR1 with IC50 values of 2 μM and 0.4 μM, respectively.
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