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LUF6283 is a partial agonist of GPR109A/HCA2 G protein-coupled receptors (Ki = 0.55 μM in a radioligand binding assay).1 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.
WARNING This product is not for human or veterinary use.
1. Effects of pyrazole partial agonists on HCA2-