TPPU - CAS 1222780-33-7
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
TTPU is a soluble epoxide hydrolase inhibitor (sEHI) (IC50= 37, 2.8 nM and 3.7 nM for monkey, mouse and human sEH, respectively) with anti-inflammatory, anti-hypertensive, neuroprotective, and cardioprotective effects.
Brife Description:
A soluble epoxide hydrolase (sEH) inhibitor (IC50= 3.7 nM for human she)
DMSO: ≥ 28 mg/mL
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
448.9±45.0 ℃ at 760 Torr
Melting Point:
195-196 ℃
1.31±0.1 g/cm3
Canonical SMILES:
1.Anti-Ulcer Efficacy of Soluble Epoxide Hydrolase Inhibitor TPPU on Diclofenac-Induced Intestinal Ulcers.
Goswami SK;Wan D;Yang J;Trindade da Silva CA;Morisseau C;Kodani SD;Yang GY;Inceoglu B;Hammock BD J Pharmacol Exp Ther. 2016 Jun;357(3):529-36. doi: 10.1124/jpet.116.232108. Epub 2016 Mar 17.
Proton pump inhibitors such as omeprazole (OME) reduce the severity of gastrointestinal (GI) ulcers induced by nonsteroidal anti-inflammatory drugs (NSAIDs) but can also increase the chance of dysbiosis. The aim of this study was to test the hypothesis that preventive use of a soluble epoxide hydrolase inhibitor (sEHI) such as TPPU can decrease NSAID-induced ulcers by increasing anti-inflammatory epoxyeicosatrienoic acids (EETs). Dose- [10, 30, and 100 mg/kg, by mouth (PO)] and time-dependent (6 and 18 hours) ulcerative effects of diclofenac sodium (DCF, an NSAID) were studied in the small intestine of Swiss Webster mice. Dose-dependent effects of TPPU (0.001-0.1 mg/kg per day for 7 days, in drinking water) were evaluated in DCF-induced intestinal toxicity and compared with OME (20 mg/kg, PO). In addition, the effect of treatment was studied on levels of Hb in blood, EETs in plasma, inflammatory markers such as myeloperoxidase (MPO) in intestinal tissue homogenates, and tissue necrosis factor-α (TNF-α) in serum. DCF dose dependently induced ulcers that were associated with both a significant (P < 0.05) loss of Hb and an increase in the level of MPO and TNF-α, with severity of ulceration highest at 18 hours.
2.Oral treatment of rodents with soluble epoxide hydrolase inhibitor 1-(1-propanoylpiperidin-4-yl)-3-[4-(trifluoromethoxy)phenyl]urea (TPPU): Resulting drug levels and modulation of oxylipin pattern.
Ostermann AI;Herbers J;Willenberg I;Chen R;Hwang SH;Greite R;Morisseau C;Gueler F;Hammock BD;Schebb NH Prostaglandins Other Lipid Mediat. 2015 Sep;121(Pt A):131-7. doi: 10.1016/j.prostaglandins.2015.06.005. Epub 2015 Jun 25.
Epoxides from polyunsaturated fatty acids (PUFAs) are potent lipid mediators. In vivo stabilization of these epoxides by blockade of the soluble epoxide hydrolase (sEH) leads to anti-inflammatory, analgesic and normotensive effects. Therefore, sEH inhibitors (sEHi) are a promising new class of drugs. Herein, we characterized pharmacokinetic (PK) and pharmacodynamic properties of a commercially available potent sEHi 1-(1-propanoylpiperidin-4-yl)-3-[4-(trifluoromethoxy)phenyl]urea (TPPU). Cell culture studies suggest its high absorption and metabolic stability. Following administration in drinking water to rats (0.2, 1, and 5mg TPPU/L with 0.2% PEG400), TPPU's blood concentration increased dose dependently within the treatment period to reach an almost steady state after 8 days. TPPU was found in all the tissues tested. The linoleic epoxide/diol ratios in most tissues were dose dependently increased, indicating significant sEH inhibition. Overall, administration of TPPU with the drinking water led to systemic distribution as well as high drug levels and thus makes chronic sEH inhibition studies possible.
3.The effects of sEH inhibitor on depression-like behavior and neurogenesis in male mice.
Wu Q;Cai H;Song J;Chang Q J Neurosci Res. 2017 Dec;95(12):2483-2492. doi: 10.1002/jnr.24080. Epub 2017 Jul 12.
Currently antidepressants take several weeks to be effective, which is one of the main reasons why patients with depression quit therapy. In the present study, we examine the acute and subacute effects of soluble epoxide hydolase (sEH) inhibitor (sEHI), a compound shown to have antidepressant effects, on mice. We found that acute administration of sEHI TPPU decreases immobility time in the forced swimming test and reduces latency to feed in the novelty suppressed-feeding test in adult male mice. Intraperitoneal administration of TPPU for seven days also increased interaction time of socially defeated mice in the social defeat test. Hippocampal BDNF expression and cell proliferation in the dentate gyrus increased six and 24 hours after TPPU treatment, respectively. Improvement in antidepressant behavior and cell proliferation were inhibited by BDNF-trkB antagonist K252a, which suggests that anti-depressant effects of sEHI may be involved in BDNF signaling. Taken together, our findings suggest that sEHI may provide a rapid antidepressant effect through alterations to BDNF-trkB signaling in the hippocampus and may provide an alternative to current slow-acting antidepressants.;© 2017 Wiley Periodicals, Inc.
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CAS 1222780-33-7 TPPU

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