LEI 101 hydrochloride
Chemical Name: 3-Cyclopropyl-1-[[4-[6-[(1,1-dioxido-4-thiomorpholinyl)methyl]-5-fluoro-2-pyridinyl]phenyl]methyl]-2,4-imidazolidinedione hydrochloride
Biological ActivityPotent and selective CB2 partial agonist (pEC50 = 8.0). Exhibits >100-fold selectivity for CB2 over CB1 and no significant interaction with hFAAH, MAGL, DAGL or NAPE-PLD. Displays antinociceptive activity in a rat neuropathic pain model and attenuates renal inflammation in a mouse kidney damage model. Orally bioavailable with low brain penetration.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery and optimization of 1-(4-(pyridin-2-yl)benzyl)imidazolidine-2,4-dione derivatives as a novel class of selective cannabinoid CB2 receptor agonists.
van der Stelt M et al.
The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity.
Mukhopadhyay et al.
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