1. Metabolic Enzyme/Protease
  2. Epoxide Hydrolase
  3. TPPU

TPPU 

Cat. No.: HY-101294 Purity: 99.01%
Handling Instructions

TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.

For research use only. We do not sell to patients.

TPPU Chemical Structure

TPPU Chemical Structure

CAS No. : 1222780-33-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 144 In-stock
Estimated Time of Arrival: December 31
25 mg USD 288 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 864 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

TTPU is a soluble epoxide hydrolase (sEH) inhibitor with IC50 values of 37 and 3.7 nM for monkey and human sEH, respectively.

IC50 & Target

IC50: 37 nM (Monkey sEH), 3.7 nM (Human sEH)[1]

In Vitro

Soluble epoxide hydrolase inhibitors (sEHIs) possess anti-inflammatory, antiatherosclerotic, antihypertensive and analgesic properties[1]. In the Caco-2 cells permeability assay, TPPU rapidly passes the cell monolayer, suggesting it will have a good intestinal permeability[2].

In Vivo

TPPU is suitable for investigating soluble epoxide hydrolase biology and the role of epoxide-containing lipids in modulating inflammatory diseases. TPPU displays high plasma concentrations when dosed orally at 0.3 mg/kg and drug-like properties. The Cmax increases with dose from 0.3 to 3 mg/kg for TPPU[1]. Following administration in drinking water to rats (0.2, 1, and 5 mg TPPU/L with 0.2% PEG400), TPPU’s blood concentration increases dose dependently within the treatment period to reach an almost steady state after 8 days[2]. The sEH inhibitor, TPPU, shows antidepressant effects in animal models of depression. Expression of sEH protein is increased in the brain of chronically stressed mice and depressed patients. Prophylactic sEH inhibition or sEH-KO results in resilience to repeated social defeat stress, associated with increased BDNF-TrkB signaling in prefrontal cortex and hippocampus of KO mice[3].

Molecular Weight

359.34

Formula

C₁₆H₂₀F₃N₃O₃

CAS No.

1222780-33-7

SMILES

O=C(NC1=CC=C(OC(F)(F)F)C=C1)NC2CCN(C(CC)=O)CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (77.92 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7829 mL 13.9144 mL 27.8288 mL
5 mM 0.5566 mL 2.7829 mL 5.5658 mL
10 mM 0.2783 mL 1.3914 mL 2.7829 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.96 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.96 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.96 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[2]

Cell monolayers that exceeds a resistance of 300 Ω cm-2 are incubated with either 1 μM or 10 μM of TPPU solution in DMSO on the apical side. Medium samples on the apical and basolateral side are collected and frozen immediately after 1, 3 and 6 hours. The apparent permeability coefficient is calculated for t=1 h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1][2]

Rats: Water is provided ad libitum containing 0.2% PEG400 with and without TPPU at a concentration of 0.2 mg/L, 1 mg/L and 5 mg/L during the treatment period (8 days). Before (0 h) and after 2 h, 4 h, 8 h, 1 d, 2 d, 4 d and 8 d, 10 μL blood are sampled from the tail vain. The blood is directly mixed with 50 μL deionzed water28 and frozen until analysis. On day 8, the animals are sacrificed by cardiac puncture after anesthesia. Plasma and whole blood are sampled[2].

Monkeys: TPPU is prepared in 0.3, 1 and 3 mg/kg doses and is administered to four animals with 48 h dosing intervals based on the t1/2 of the compound obtained from the first cassette dosing. Blood is collected from animals at time points 0, 0.25, 0.5, 1, 2, 3, 4, 8, 24 and 48 h after each dosing for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

TPPUEpoxide HydrolaseInhibitorinhibitorinhibit

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