TPPU


Catalog No. Size PriceQuantity
M22485-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

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 . 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 . Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 1222780-33-7

Molecular Weight: 359.34

Formula: C16H20F3N3O3

Chemical Name: 3-(1-propanoylpiperidin-4-yl)-1-[4-(trifluoromethoxy)phenyl]urea

Smiles: CCC(=O)N1CCC(CC1)NC(=O)NC1C=CC(=CC=1)OC(F)(F)F

InChiKey: AAJMQTLFRTZCJK-UHFFFAOYSA-N

InChi: InChI=1S/C16H20F3N3O3/c1-2-14(23)22-9-7-12(8-10-22)21-15(24)20-11-3-5-13(6-4-11)25-16(17,18)19/h3-6,12H,2,7-10H2,1H3,(H2,20,21,24)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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