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FT113

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Chemical Structure| 1630808-89-7 同义名 : -
CAS号 : 1630808-89-7
货号 : A1149113
分子式 : C22H20FN3O4
纯度 : 99%+
分子量 : 409.41
MDL号 : MFCD31813811
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(146.55 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The fatty acids are synthesized by a number of decarboxylative Claisen condensation reactions from acetyl-CoA and malonyl-CoA. Fatty acid synthase is a multi-enzyme protein which is to catalyze the synthesis of palmitate (C16:0, a long-chain saturated fatty acid) from acetyl-CoA and malonyl-CoA, in the presence of NADPH. FT113 is a novel potent inhibitor of fatty acid synthase (fasn) with IC50 of 213 nM, which also displays excellent cellular activity(Mv411 cell IC50=26nM) [1]. The pharmacokinetic properties of FT113 were assessed in mice, and FT113 showed no acute toxicity and provided excellent exposure when dosed orally at 5 mg/kg. Also upon oral dosing at 5 mg/kg in male Sprague-Dawley rats, FT113 displayed excellent exposure and bioavailability[1] .
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.44mL

0.49mL

0.24mL

12.21mL

2.44mL

1.22mL

24.43mL

4.89mL

2.44mL
参考文献

[1]Martin MW, Lancia DR Jr, Li H, Schiller SER, Toms AV, Wang Z, Bair KW, Castro J, Fessler S, Gotur D, Hubbs SE, Kauffman GS, Kershaw M, Luke GP, McKinnon C, Yao L, Lu W, Millan DS. Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN). Bioorg Med Chem Lett. 2019 Apr 15;29(8):1001-1006. doi: 10.1016/j.bmcl.2019.02.012. Epub 2019 Feb 11. PMID: 30803804.