LEI 101 hydrochloride
Potent 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.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 508.99. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.96 mL||9.82 mL||19.65 mL|
|5 mM||0.39 mL||1.96 mL||3.93 mL|
|10 mM||0.2 mL||0.98 mL||1.96 mL|
|50 mM||0.04 mL||0.2 mL||0.39 mL|
References are publications that support the biological activity of the product.
van der Stelt M et al (2011) 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. J.Med.Chem. 54 7350 PMID: 21923175
Mukhopadhyay et al (2016) The novel, orally available and peripherally restricted selective cannabinoid CB2 receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity. Br.J.Pharmacol. 173 446 PMID: 26398481
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