TPPU
目录号 : GC15387
TPPU是一种可溶性环氧化物水解酶(sEH)抑制剂，对猴和人sEH的IC50值分别为37和3.7 nM。
Cas No.:1222780-33-7
Sample solution is provided at 25 µL, 10mM.
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TPPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH. TPPU has anti-inflammatory, analgesic, antiatherogenic and antihypertensive effects[1-2].
TPPU(1–10 μM; 48 h) reversed CORT-induced cell death in PC12 cells[3]. TPPU(0.1–10 μM; 24 h) protects tau from H2O2-induced hyperphosphorylation in HEK293/tau cells by regulating PI3K/AKT/GSK-3β pathway[4].
TPPU (i.p.; 10 mg/kg) treatment decreases serum dihydroxyeicosatrienoic acid (DHET) levels and serum IL-6 levels following burn injury, preventing DHET induced neutrophil depression in burn injury mice model [5]. TPPU(0-5 mg/L TPPU; delivered in drinking water; 1 week) increased exercise-induced effects on inhibiting cardiac enlargement and improving cardiac function by increasing EET levels in MI mice[6]. Pre-treatment with TPPU(0.1 mg/kg/d; i.g) attenuated seizures severity during status epilepticus (SE) and depressive behaviours during the period of epileptogenesis[7].
References:
[1]. Ulu A, Appt S, et,al. Pharmacokinetics and in vivo potency of soluble epoxide hydrolase inhibitors in cynomolgus monkeys. Br J Pharmacol. 2012 Mar;165(5):1401-12. doi: 10.1111/j.1476-5381.2011.01641.x. PMID: 21880036; PMCID: PMC3372725.
[2]. Li J, Wen Z, et,al. Soluble epoxide hydrolase inhibitor promotes the healing of oral ulcers. Clinics (Sao Paulo). 2023 May 4;78:100208. doi: 10.1016/j.clinsp.2023.100208. PMID: 37148830; PMCID: PMC10192938.
[3]. Wu Q, Song J, et,al. TPPU, a sEH Inhibitor, Attenuates Corticosterone-Induced PC12 Cell Injury by Modulation of BDNF-TrkB Pathway. J Mol Neurosci. 2019 Mar;67(3):364-372. doi: 10.1007/s12031-018-1230-z. Epub 2019 Jan 14. PMID: 30644034.
[4]. Yao ES, Tang Y, et,al. TPPU protects tau from H2O2-induced hyperphosphorylation in HEK293/tau cells by regulating PI3K/AKT/GSK-3β pathway. J Huazhong Univ Sci Technolog Med Sci. 2016 Dec;36(6):785-790. doi: 10.1007/s11596-016-1662-z. Epub 2016 Dec 7. PMID: 27924507.
[5]. Bergmann CB, Hammock BD, et,al. TPPU treatment of burned mice dampens inflammation and generation of bioactive DHET which impairs neutrophil function. Sci Rep. 2021 Aug 16;11(1):16555. doi: 10.1038/s41598-021-96014-2. PMID: 34400718; PMCID: PMC8368302.
[6]. Guo Y, Luo F, et,al. TPPU enhanced exercise-induced epoxyeicosatrienoic acid concentrations to exert cardioprotection in mice after myocardial infarction. J Cell Mol Med. 2018 Mar;22(3):1489-1500. doi: 10.1111/jcmm.13412. Epub 2017 Dec 19. PMID: 29265525; PMCID: PMC5824362.
[7]. Peng W, Shen Y et,al. TPPU Pre-Treatment Rescues Dendritic Spine Loss and Alleviates Depressive Behaviours during the Latent Period in the Lithium Chloride-Pilocarpine-Induced Status Epilepticus Rat Model. Brain Sci. 2021 Nov 5;11(11):1465. doi: 10.3390/brainsci11111465. PMID: 34827464; PMCID: PMC8615907.
TPPU是一种可溶性环氧化物水解酶(sEH)抑制剂，对猴和人sEH的IC50值分别为37和3.7 nM。TPPU具有抗炎、镇痛、抗动脉粥样硬化、降压等作用[1-2]。
TPPU (1–10 μM; 48 h)逆转CORT诱导的PC12细胞死亡[3]。TPPU (0.1–10 μM; 24 h)通过调节PI3K/AKT/GSK-3β通路，保护HEK293/tau细胞中H2O2诱导的tau过度磷酸化[4]。
TPPU (i.p.; 10 mg/kg) 处理可降低烧伤后小鼠血清dihydroxyeicosatrienoic acid (DHET)水平和血清IL-6水平，预防DHET诱导的烧伤模型小鼠中性粒细胞抑制 [5]。TPPU (0-5 mg/L TPPU; delivered in drinking water; 1 week)通过提高心肌梗死小鼠EET水平，增强运动诱导的抑制心肌扩大和改善心功能的作用[6]。TPPU (0.1 mg/kg/d; i.g)预处理可减轻癫痫持续状态期间癫痫发作的严重程度和癫痫发生期间的抑郁行为[7]。
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Cell experiment [1]: |
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Cell lines |
PC12 cells |
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Preparation method |
PC12 cells were exposed to 200 μM CORT for 48 h and then with 1-10 μM TPPU. |
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Reaction Conditions |
1-10 μM; 48 h |
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Applications |
TPPU reversed CORT-induced cell death in PC12 cells. |
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Animal experiment [2]: |
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Animal models |
C57BL/6 mice |
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Preparation method |
Myocardial infarction(MI) mouse model was established. After 1 week recovery, the surviving mice were randomly divided into four groups: non-myocardial infarction and non-exercise training (NMI NET), non-myocardial infarction with exercise training (NMI ET), myocardial infarction and non-exercise training (MI NET), and myocardial infarction with exercise training (MI ET).Mice in the ET groups underwent 4 weeks of exercise. To test the effect of TPPU on exercised mice, mice in the MI ET group were fed 0, 0.2, 1 or 5 mg/L TPPU for 1 week prior to the MI surgery and subsequent 4-week exercise programme. |
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Dosage form |
0-5 mg/L TPPU; delivered in drinking water; 1 week |
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Applications |
TPPU increased exercise-induced effects on inhibiting cardiac enlargement and improving cardiac function by increasing epoxyeicosatrienoic acid (EET) levels in MI mice. |
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References: [1]. Wu Q, Song J,et,al. TPPU, a sEH Inhibitor, Attenuates Corticosterone-Induced PC12 Cell Injury by Modulation of BDNF-TrkB Pathway. J Mol Neurosci. 2019 Mar;67(3):364-372. doi: 10.1007/s12031-018-1230-z. Epub 2019 Jan 14. PMID: 30644034. [2]. Guo Y, Luo F et,al. TPPU enhanced exercise-induced epoxyeicosatrienoic acid concentrations to exert cardioprotection in mice after myocardial infarction. J Cell Mol Med. 2018 Mar;22(3):1489-1500. doi: 10.1111/jcmm.13412. Epub 2017 Dec 19. PMID: 29265525; PMCID: PMC5824362. |
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| Cas No. | 1222780-33-7 | SDF | |
| 化学名 | N-[1-(1-oxopropyl)-4-piperidinyl]-N’-[4-(trifluoromethoxy)phenyl)-urea | ||
| Canonical SMILES | CCC(N(CC1)CCC1NC(NC2=CC=C(OC(F)(F)F)C=C2)=O)=O | ||
| 分子式 | C16H20F3N3O3 | 分子量 | 359.3 |
| 溶解度 | ≤5mg/ml in ethanol;12.5mg/ml in DMSO;15mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7832 mL | 13.9159 mL | 27.8319 mL |
| 5 mM | 0.5566 mL | 2.7832 mL | 5.5664 mL |
| 10 mM | 0.2783 mL | 1.3916 mL | 2.7832 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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