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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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TTPU is a novel and potent soluble epoxide hydrolase (sEH) inhibitor with anti-inflammatory effects. It has an IC50 of 37 and 3.7 nM for monkey and human sEH, respectively.
ln Vitro |
Soluble epoxide rapid enzyme conjugation (sEHI) possesses anti-inflammatory, anti-atherosclerotic, anti-hypertensive and analgesic properties [1]. In the Caco-2 cell permeability assay, TPPU went through the cell monolayer, showing that it has good destruction permeability [2].
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ln Vivo |
The biology of soluble epoxide resting enzymes and the function of epoxide-containing rosettes in regulatory regulation can both be studied with TPPU. At a dosage of 0.3 mg/kg, TPPU exhibited high rose concentration and drug-like characteristics. Cmax for TPPU rises from 0.3 to 3 mg/kg with dosage [1]. The blood concentration of TPPU showed a dose-dependent rise after treatment following incubation in water (0.2, 1 and 5 mg TPPU/L with 0.2% PEG400) and reached an almost steady condition after 8 days [2]. Animal models of depression show antidepressant benefits from sEH reverse TPPU. sEH preventative sEH inhibition or sEH-KO results in recovery from the stress of repeated social defeat in the brains of chronic intermittent and depressed patients and is linked to enhanced BDNF-TrkB signaling in the KO prefrontal layer and hippocampus [3].
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References |
[1]. Ulu A, et al. Pharmacokinetics and in vivo potency of soluble epoxide hydrolase inhibitors in cynomolgus monkeys. Br J Pharmacol. 2012 Mar;165(5):1401-12.
[2]. Ostermann AI, et al. 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. Prostaglandins Other Lipid Mediat. 2015 Sep;121(Pt A):131-7. [3]. Ren Q, et al. Gene deficiency and pharmacological inhibition of soluble epoxide hydrolase confers resilience to repeated social defeat stress. Proceedings of the National Academy of Sciences of the United States of America (2016), 113(13), E1944-E1952 |
Molecular Formula |
C16H20N3O3F3
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Molecular Weight |
359.3435
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CAS # |
1222780-33-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(NC1=CC=C(OC(F)(F)F)C=C1)NC2CCN(C(CC)=O)CC2
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~231.90 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.