TPPU

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Chemical Structure| 1222780-33-7 同义名 : -
CAS号 : 1222780-33-7
货号 : A982864
分子式 : C16H20F3N3O3
纯度 : 99%+
分子量 : 359.34
MDL号 : MFCD26142949
存储条件：

Pure form Inert atmosphere, room temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(236.54 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
生物活性
描述 The soluble epoxide hydrolase (sEH) converts epoxides to diols by catalytic addition of a water molecule. It has been shown to metabolize fatty acid epoxides in various human diseases. TPPU is a potent sEH inhibitor with IC50 values of 3.7 and 2.8nM for human and murine sHE, respectively[1]. TPPU also shows inhibitory activity against monkey sEH with an IC50 value of 37nM[2]. TPPU binds to recombinant human sEH with a Ki value of 0.9±0.1nM and koff of 10.5×10-4/s. Administration of rats with 10mg/kg TPPU via oral gavage inhibited human sEH with an IC50 value of 1.1±0.1nM[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.83mL

5.57mL

2.78mL
参考文献

[1]Rose TE, Morisseau C, Liu JY, et al. 1-Aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain. J Med Chem. 2010;53(19):7067-7075. doi:10.1021/jm100691c

[2]Ulu A, Appt S, Morisseau C, et al. Pharmacokinetics and in vivo potency of soluble epoxide hydrolase inhibitors in cynomolgus monkeys. Br J Pharmacol. 2012;165(5):1401-1412. doi:10.1111/j.1476-5381.2011.01641.x

[3]Wan D, Yang J, McReynolds CB, et al. In vitro and in vivo Metabolism of a Potent Inhibitor of Soluble Epoxide Hydrolase, 1-(1-Propionylpiperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea. Front Pharmacol. 2019;10:464. doi:10.3389/fphar.2019.00464