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TPPU

Catalog No. T7199   CAS 1222780-33-7

TPPU is a potent inhibitor of both human and mouse sEH (IC50 of 3.7 and 2.8 nM, respectively)

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TPPU Chemical Structure
TPPU, CAS 1222780-33-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 32.00
5 mg In stock $ 67.00
10 mg In stock $ 117.00
25 mg In stock $ 237.00
50 mg In stock $ 389.00
100 mg In stock $ 569.00
1 mL * 10 mM (in DMSO) In stock $ 74.00
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Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TPPU is a potent inhibitor of both human and mouse sEH (IC50 of 3.7 and 2.8 nM, respectively)
Targets&IC50 sEH (human):3.7 nM , sEH (mouse):2.8 nM
In vivo TPPU and two 4-(cyclohexyloxy) benzoic acid urea sEHIs displayed high plasma concentrations (>10 × IC(50)), when dosed orally at 0.3 mg·kg(-1). Although the 4-(cyclohexyloxy) benzoic acid ureas were more potent against monkey sEH than piperidyl ureas (TPAU and TPPU), the latter compounds showed higher plasma concentrations and more drug-like properties. The C(max) increased with dose from 0.3 to 3 mg·kg(-1) for TPPU and from 0.1 to 3 mg·kg(-1) for TPAU, although it was not linear over this range of doses. As an indication of target engagement, ratios of linoleate epoxides to diols increased with TPPU administration[1].
Animal Research PK parameters of 11 sEHIs in cynomolgus monkeys were determined after oral dosing with 0.3 mg/kg. Their physical properties and inhibitory potency in hepatic cytosol of cynomolgus monkeys were examined. Dose-dependent effects of the two inhibitors 1-trifluoromethoxyphenyl-3-(1-propionylpiperidin-4-yl) urea (TPPU) and the related acetyl piperidine derivative, 1-trifluoromethoxyphenyl-3-(1-acetylpiperidin-4-yl) urea (TPAU), on natural blood eicosanoids[1]
Molecular Weight 359.34
Formula C16H20F3N3O3
CAS No. 1222780-33-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 28 mg/mL (77.92 mM)

TargetMolReferences and Literature

1. Pharmacokinetics and in vivo potency of soluble epoxide hydrolase inhibitors in cynomolgus monkeys[J]. British Journal of Pharmacology, 2012, 165. 2. Yao ES, Tang Y, Liu XH,et al.TPPU protects tau from H2O2-induced hyperphosphorylation in HEK293/tau cells by regulating PI3K/AKT/GSK-3β pathway[J].J Huazhong Univ Sci Technolog Med Sci. 2016 Dec;36(6):785-790.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library Inhibitor Library Covalent Inhibitor Library Bioactive Compound Library Metabolism Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Immunology/Inflammation Compound Library

Related Products

Related compounds with same targets
(Rac)-EC5026 CUDA GSK2256294A sEH inhibitor-7 ARM1 1,3-Diphenylurea sEH inhibitor-16 Diflapolin

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Keywords

TPPU 1222780-33-7 Metabolism Epoxide Hydrolase inhibit Inhibitor inhibitor

 

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