| Bioactivity | BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats[1][2]. | ||||||||||||
| Target | IC50: 79 nM (FASN) | ||||||||||||
| Invitro | BI 99179 is potent in the mouse hypothalamic N-42 cell with an IC50 of 0.6 μM. BI 99179 shows no significant LDH release in the cytotoxicity assay up to 30 μM[1].BI 99179 (BI-99179; 1, 2, and 4 µM) shows antiproliferative efficacy in human glioma GAMG cells[2]. Cell Proliferation Assay[2] Cell Line: | ||||||||||||
| In Vivo | BI 99179 has a super pharmacokinetic profile in male Han/Wistar rats (oral application of 4 mg/kg) with half life (t1/2) of 3.0 h[1]. | ||||||||||||
| Name | BI 99179 | ||||||||||||
| CAS | 1291779-76-4 | ||||||||||||
| Formula | C23H25N3O3 | ||||||||||||
| Molar Mass | 391.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kley JT, et al. Discovery of BI 99179, a potent and selective inhibitor of type I fatty acid synthase with central exposure.Bioorg Med Chem Lett. 2011 Oct 1;21(19):5924-7. [2]. Prosanta K Singha, et al. Evaluation of FASN inhibitors by a versatile toolkit reveals differences in pharmacology between human and rodent FASN preparations and in antiproliferative efficacy in vitro vs. in situ in human cancer cells. Eur J Pharm Sci. 20 |