GPR

The protective effects of NE 52-QQ57 against interleukin-33-induced inflammatory response in activated synovial mast cells

67 views | Oct 09 2023

The study suggests that inhibiting GPR4 signaling with the antagonist NE 52-QQ57 may have therapeutic benefits in rheumatoid arthritis by reducing inflammatory responses and oxidative stress in synovial mast cells. [Read the Full Post]

Investigation of the Pharmacokinetics and Metabolic Fate of Fasiglifam (TAK-875) in Male and Female Rats Following Oral and Intravenous Administration

96 views | Mar 27 2023

Fasiglifam has good oral bioavailability and is extensively metabolized in rats, with a novel biotransformation observed and sex-related differences in drug elimination. [Read the Full Post]

Modeling drug-induced liver injury and screening for anti-hepatofibrotic compounds using human PSC-derived organoids

121 views | Mar 27 2023

Human liver organoids derived from pluripotent stem cells have the potential to serve as a preclinical model for drug safety testing and anti-fibrotic drug screening. [Read the Full Post]

Central Agonism of GPR120 Acutely Inhibits Food Intake and Food Reward and Chronically Suppresses Anxiety-Like Behavior in Mice

886 views | Aug 23 2018

Auguste S et al. suggested that GPR120 could mediate the effects of central ω-3 polyunsaturated fatty acids to inhibit appetite. The anxiolytic effect elicited by GPR120 agonist infusions favors the testing of compounds that can enter the brain to activate GPR120 for the mitigation of anxiety. [Read the Full Post]

A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice

1142 views | Mar 30 2018

Zheng C et al. demonstrated that TGR5 activator WB403 effectively promoted GLP-1 release, improved hyperglycemia and preserved the mass and function of pancreatic β-cells, whereas it did not show a significant side effect on gallbladder. [Read the Full Post]

TAK 875 was dissolved in dimethyl sulfoxide

2979 views | Feb 12 2014

AK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. [Read the Full Post]