TPPU

SKU: orb1299986

Description

TPPU

Research Area

Metabolism Research

Key Properties

• CAS Number: 1222780-33-7
• MW: 359.34
• Purity: 98.00%
• Formula: C₁₆H₂₀F₃N₃O₃
• SMILES: CCC(=O)N1CCC(CC1)NC(=O)Nc1ccc(OC(F)(F)F)cc1
• Target: Epoxide Hydrolase
• Solubility: DMSO:28 mg/mL (77.92 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.57 mM)

Bioactivity

• Target 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.
• 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

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, EpoxideHydrolase, Epoxide Hydrolase, Inhibitor, sEH, TPPU

Compound Identifiers

PubChem CID

44142782