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TPPU {[allProObj[0].p_purity_real_show]}

货号:A982864

TPPU是一种环氧化物水解酶(sEH)抑制剂,IC50 为 3.7 nM,具有抗炎和抗动脉粥样硬化的活性。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
TPPU 化学结构 CAS号:1222780-33-7
TPPU 化学结构
CAS号:1222780-33-7
TPPU 3D分子结构
CAS号:1222780-33-7
TPPU 化学结构 CAS号:1222780-33-7
TPPU 3D分子结构 CAS号:1222780-33-7
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TPPU 纯度/质量文件 产品仅供科研

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TPPU 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].

TPPU 细胞实验

Cell Line
Concentration Treated Time Description References
Beas-2B cells 10 µM 24 hours TPPU reduced TGF-β1-induced fibronectin expression Exp Mol Med. 2021 May;53(5):864-874
A549 cells 20 µM 48 hours TPPU reduced the number of BLM-induced β-gal positive cells. Redox Biol. 2023 Jul;63:102765
Mixed mouse glial cultures 10 µM 30 minutes To evaluate the effect of TPPU on mixed glial inflammation, results showed that TPPU suppressed microglial reactivity through astrocytes. Sci Transl Med. 2020 Dec 9;12(573):eabb1206
Mouse primary microglia 10 µM 30 minutes To evaluate the effect of TPPU on microglial inflammation, results showed that TPPU had no direct effect on microglia. Sci Transl Med. 2020 Dec 9;12(573):eabb1206
Mouse primary astrocytes 0.5 µM to 10 µM 30 minutes To evaluate the effect of TPPU on LPS-induced inflammation, results showed that TPPU dose-dependently reduced nitrite release and pro-inflammatory molecule expression. Sci Transl Med. 2020 Dec 9;12(573):eabb1206
MLE12 cells 20 µM 48 hours TPPU significantly reduced the number of BLM-induced β-gal positive cells and reduced the expression of senescence-related p53 and p21 proteins in MLE12 cells. Redox Biol. 2023 Jul;63:102765

TPPU 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Bleomycin-induced pulmonary fibrosis model Intraperitoneal injection 0.25 mg/kg 5 days per week for 3 weeks TPPU significantly attenuated bleomycin-induced pulmonary fibrosis and reduced collagen levels Exp Mol Med. 2021 May;53(5):864-874
Mice Inflammation and social defeat stress models Oral 0.3, 1.0, or 3.0 mg/kg Single administration or continuous administration for 3 weeks TPPU showed rapid antidepressant effects in both inflammation and social defeat stress models, preventing and alleviating depression-like behaviors. Proc Natl Acad Sci U S A. 2016 Mar 29;113(13):E1944-52
Mice MPTP-induced neurotoxicity model Oral 0.3, 1.0, or 3.0 mg/kg Twice daily from day 2 to day 7 TPPU significantly attenuated MPTP-induced dopaminergic neurotoxicity in the striatum and substantia nigra Proc Natl Acad Sci U S A. 2018 Jun 19;115(25):E5815-E5823
C57BL/6J mice D-galactose-induced premature aging mouse model Intraperitoneal injection 1 mg/kg Once daily for six weeks TPPU significantly inhibited the protein expression of p16, p21, and γH2AX in D-gal-induced premature aging mice and reduced the degree of age-related pulmonary fibrosis. Redox Biol. 2023 Jul;63:102765
Male C57BL/6N mice Scald injury model Intraperitoneal injection 10 mg/kg Three administrations at 48 h, 24 h, and directly before burn injury To evaluate the effect of TPPU on DiHOME levels and immune cell necrosis in scalded mice, it was found that TPPU significantly reduced 12,13-DiHOME levels and decreased necrosis of innate and adaptive immune cells in a dose-dependent manner. Proc Natl Acad Sci U S A. 2022 Mar 29;119(13):e2120691119
Mice Maternal immune activation (MIA) model Drinking water 15 mg/L From P28 to P56 TPPU treatment prevented cognitive deficits and the reduction of PV and GAD67 immunoreactivity in the medial prefrontal cortex (mPFC) of adult offspring after MIA. Proc Natl Acad Sci U S A. 2019 Apr 2;116(14):7083-7088
C57BL/6J mice Myocardial infarction model Oral (via drinking water) 15 mg/L 3 weeks To evaluate the effect of TPPU on cardiac function and fibrosis post-myocardial infarction, results showed that TPPU significantly improved cardiac function and reduced cardiac fibrosis. Proc Natl Acad Sci U S A. 2013 Apr 2;110(14):5618-23
C57BL/6 mice PM2.5-mediated lung injury model Intragastric administration 3 mg/kg Three times per week for three weeks To evaluate the protective effect of TPPU on PM2.5-mediated lung injury. Results showed that TPPU treatment reversed PM2.5-induced pulmonary hyperemia, edema, alveolar wall thickening, and macrophage activation, reduced levels of TNF-α, IL-6, MPO, and LDH, and alleviated inflammatory responses by inhibiting the MAPK/NF-κB signaling pathway. J Hazard Mater. 2023 Sep 15;458:131890
Mice 5xFAD transgenic mice Oral gavage or drinking water 3 mg/kg 24 hours or 2.5 to 4.5 months To evaluate the effect of TPPU on acute inflammation and long-term AD pathology, results showed that TPPU reduced neuroinflammation, improved Aβ pathology, and cognitive function. Sci Transl Med. 2020 Dec 9;12(573):eabb1206
Mice Destabilization of the medial meniscus (DMM) model Intraperitoneal injection 3mg/kg Single injection, measured at 3 hours post-injection Acute TPPU injection significantly reversed DMM-induced pain behaviors, including increased weight-bearing on the ipsilateral hind-limb and reversal of the lowered ipsilateral hind-paw withdrawal thresholds. Arthritis Rheumatol. 2022 Apr;74(4):623-633

TPPU 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

TPPU 实验方案

计算器
存储液制备 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

TPPU 技术信息

CAS号1222780-33-7
分子式C16H20F3N3O3
分子量 359.34
SMILES Code O=C(NC1=CC=C(OC(F)(F)F)C=C1)NC2CCN(C(CC)=O)CC2
MDL No. MFCD26142949
别名
运输蓝冰
InChI Key AAJMQTLFRTZCJK-UHFFFAOYSA-N
Pubchem ID 44142782
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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