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| Names | |
|---|---|
| Preferred IUPAC name N-Benzyl-4-[(2-methylpropyl)amino]-2-{4-[(oxan-3-yl)methyl]piperazin-1-yl}pyrimidine-5-carboxamide | |
| Identifiers | |
3D model (JSmol) | |
| ChEMBL | |
| ChemSpider |
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| Properties | |
| C26H38N6O2 | |
| Molar mass | 466.630 g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
PF-4840154 is apyrimidine derivative discovered byPfizer at itsSandwich, Kent research center. The compound is a potent, selective activator of both the human (EC50 = 23 nM) and rat (EC50 = 97 nM)TRPA1 channels.[1] This compound elicitsnociception in a mouse model throughTRPA1 activation. PF-4840154 is used as a referenceagonist of theTRPA1 channel forin-vitrohigh-throughput screening purposes, and is superior toallyl isothiocyanate for this use.[2] TheTRPA1 channel is considered an attractive pain target based on the fact thatTRPA1 knockout mice showed near complete attenuation of pain behaviors in somepre-clinical development models.[3][4]
