TPPU
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: human and mouse sEH (IC50 = 3.7 and 2.8 nM, respectively)
TPPU is a potent inhibitor of both human and mouse sEH.
The soluble epoxide hydrolase (sEH) can convert epoxides to the corresponding diols by the catalytic addition of a water molecule. sEH is implicated in various disease states for its ability to metabolize fatty acid epoxides such as epoxyeicosatrienoic acids and leukotoxin, important endogenous signaling lipids, to less active dihydroxyeicosatrienoic acids and toxic, proinflammatory leukotoxin diols, respectively. sEH inhibitors are of growing interest for therapeutic use since they have been shown to increase the in vivo concentration of EETs and other fatty acid epoxides.
In vitro: TPPU was identified as a potent inhibitor of both human and mouse sEH with IC50 of 3.7 and 2.8 nM, respectively [1].
In vivo: Animal study found that oral administration of 13 1-aryl-3-(1-acylpiperidin-4-yl)urea inhibitors including TPPU in mice showed substantial improvements in pharmacokinetic parameters over previously reported 1-adamantylurea based inhibitors. For example, 1-(1-(cyclopropanecarbonyl)piperidin-4-yl)-3-(4-(trifluoromethoxy)phenyl)urea, a close analog of TPPU, had a 7-fold increase in potency, a 65-fold increase in Cmax, and a 3300-fold increase in AUC over its adamantine analogue 1-(1-adamantyl)-3-(1-propionylpiperidin-4-yl)urea. This sEH inhibitor displayed a 1000-fold increase in potency when compared to morphine by reducing hyperalgesia using the in vivo carrageenan induced inflammatory pain model [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Rose, T. E.,Morisseau, C.,Liu, J.Y., et al. 1-aryl-3-(1-acylpiperidin-4-yl)urea inhibitors of human and murine soluble epoxide hydrolase: Structure-activity relationships, pharmacokinetics, and reduction of inflammatory pain. J Med Chem. 2010 Oct 14;53(19):7067-75.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 359.3 |
Cas No. | 1222780-33-7 |
Formula | C16H20F3N3O3 |
Solubility | ≤5mg/ml in ethanol;12.5mg/ml in DMSO;15mg/ml in dimethyl formamide |
Chemical Name | N-[1-(1-oxopropyl)-4-piperidinyl]-N’-[4-(trifluoromethoxy)phenyl)-urea |
SDF | Download SDF |
Canonical SMILES | CCC(N(CC1)CCC1NC(NC2=CC=C(OC(F)(F)F)C=C2)=O)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
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