RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively
靶点:
Others
体内研究:
Oral administration of RR6 in Wistar rats (150-200 g) completely inhibited plasma vanin activity and caused alterations of plasma lipid concentrations upon fasting. RR6 at 3 mg/mL in rats caused a nearly complete inhibition of plasma vanin.
参考文献:
1. Jansen PA et al. Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chem Biol. 2013 Mar 15;8(3):530-4.