Application
Lipofermata may be used to evaluate fatty acidtransport inhibition in Caco-2, HepG2, and C2C12 cell lines; and to studyits effect on LPS-induced inflammatory responses in whole blood and humanmonocytes.
Biochem/physiol Actions
Lipofermata (CB-16.2) is an orally active and selective long-chain fatty acid (LCFA) transport protein FATP2 (SLC27A2) inhibitor (IC50 in μM =2.74/HepG2, 4.65/INS-1E, 5.67/C2C12, 6.09/Caco2; IC50 = 39.34 μM in non-FATP2-expressing 3T3L1) with no effect against medium chain (C6-C10) fatty acids transport by passive diffusion. Lipofermata prevents palmitate-mediated oxidative stress and cell death in cultures (5-50 μM lipofermata against 500 μM palmitate; HepG2 and INS-1E cells) and prevents the absorption of 13C-oleate in mice in vivo (300 mg/mL lipofermata p.p. 1h prior to 500 mg/kg 13C-oleate p.o.).
| Quality Segment | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to light brown |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | O=C1NC2=CC=C(C=C2C13SC(C4=CC=CC=C4)=NN3)Br |
