BI 99179
目录号: PL14888 纯度: ≥99%
CAS No. :1291779-76-4
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中文名称
BI 99179
英文名称
BI 99179
英文别名
BI99179;(1R,3S)-N-(4-(Benzo[d]oxazol-2-yl)phenyl)-N-methyl-3-propionamidocyclopentane-1-carboxamide;BDBM50354699;SB19616;BI 99179;(1R,3S)-N-(4-(Benzo[d]oxazol-2-yl)phenyl)-N-methyl-3-propionamidocyclopentanecarboxamide;(1R,3S)-N-4-(1,3-benzoxazol-2-yl)phenyl-N-methyl-3-propanamidocyclopentane-1-carboxamide
Cas No.
1291779-76-4
分子式
C23H25N3O3
分子量
391.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
BI 99179 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。BI 99179 是一种适用于体内验证 FAS 作为脂质代谢相关疾病的靶点的工具化合物。在大鼠中口服 BI 99179 表现出显着的外周和中央暴露。
生物活性
BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC 50 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.
性状
Solid
IC50 & Target[1][2]
IC50: 79 nM (FASN)
体外研究(In Vitro)
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.
BI 99179 (BI-99179; 1, 2, and 4 μM) shows antiproliferative efficacy in human glioma GAMG cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
BI 99179 has a super pharmacokinetic profile in male Han/Wistar rats (oral application of 4 mg/kg) with half life (t 1/2 ) of 3.0 h. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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
溶解度数据
In Vitro: DMSO : 125 mg/mL (319.32 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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