1-Piperazineacetamide, 4-(5-fluoro-2-pyridinyl)-N-(4,5,6,7-tetrahydro-2-benzothiazolyl)-

Biological Activity

FATP1-IN-1 is a fatty acid transport protein 1 (FATP1) inhibitor. FATP1-IN-1 is an inhibition of recombinant human or mouse acyl-CoA synthetase activity of FATP1, with the IC50 values of 0.046 μM or 0.60 μM, respectively[1]. FATP1-IN-1 (p.o.; 10 mg/kg) treatment shows the Cmax, AUC and Tmax were 5.5 μg/mL, 36 μg h/mL and 0.33 hours, respectively, and exceeds the mouse IC50 value of 0.22 μM without considering plasma protein binding.

References

[1]. Matsufuji T, et al. Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties. Bioorg Med Chem Lett. 2013;23(9):2560-2565.