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BI99179 是一种有效的选择性 I 型脂肪酸合成酶 (FAS) 抑制剂,IC50 为 79 nM。在大鼠中口服 BI 99179 表现出显着的外周和中央暴露。
BI99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats[1].
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 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].
[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.
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