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LUF6283 is a partial agonist of GPR109A/HCA₂ G protein-coupled receptors (K_i = 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.

LUF 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.

[1] ZHAOSHA LI. Effects of pyrazole partial agonists on HCA2-mediated flushing and VLDL-triglyceride levels in mice[J]. British Journal of Pharmacology, 2012, 167 4: 818-825. DOI: 10.1111/j.1476-5381.2012.02039.x