FXR agonist 17 functions as a steroidal agonist of the farnesoid X receptor (FXR), exhibiting EC50 values of 42.2 nM in TR-FRET assays and 176.4 nM in luciferase reporter assays. This compound also activates TGR5 with an EC50 of 2.6 μM while showing no activation of hMRGPRX4. FXR agonist 17 demonstrates significant biological activity through its anti-inflammatory, hepatoprotective, and antifibrotic properties, contributing to the reduction of non-alcoholic steatohepatitis (NAFLD) activity scores and alleviating liver fibrosis severity. It serves as a valuable tool for research into NAFLD, cholestatic liver disease, and liver fibrosis.
FXR agonist 17 functions as a steroidal agonist of the farnesoid X receptor (FXR), exhibiting EC50 values of 42.2 nM in TR-FRET assays and 176.4 nM in luciferase reporter assays. This compound also activates TGR5 with an EC50 of 2.6 μM while showing no activation of hMRGPRX4. FXR agonist 17 demonstrates significant biological activity through its anti-inflammatory, hepatoprotective, and antifibrotic properties, contributing to the reduction of non-alcoholic steatohepatitis (NAFLD) activity scores and alleviating liver fibrosis severity. It serves as a valuable tool for research into NAFLD, cholestatic liver disease, and liver fibrosis.
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