5-Butyl-1H-pyrazole-3-carboxylic acid

BeschreibungLUF6283 is a partial agonist of GPR109A/HCA2 G protein-coupled receptors (Ki = 0.55 μM in a radioligand binding assay). It stimulates [35S]-GTPγS binding and increases phosphorylation of ERK in HEK293T cells expressing GPR109A/HCA2 receptors (EC50s = 3.1 and 0.32 μM, respectively). In vivo, LUF6283 (400 mg/kg per day) reduces plasma levels of VLDL and hepatic expression of apolipoprotein B in mice.

VerwendenLUF 6283 is a partial agonist of HCA2 and is a promising drug candidate to achieve a beneficial lipid lowering effect of niacin, ultimately treating dyslipidemic disorders.