Bioactivity | LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors[1][2]. |
In Vivo | LEI-101 (2, 6, and 20 mg/kg, po) shows in vivo activity in a spinal nerve ligation model of neuropathic pain in rats[1].LEI‐101 (p.o. or i.p.) at 3 or 10 mg/kg dose-dependently prevents kidney dysfunction and/or morphological damage induced by cisplatin in mice[2]. Animal Model: |
Name | LEI-101 |
CAS | 2250025-91-1 |
Formula | C23H26ClFN4O4S |
Molar Mass | 508.99 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Mario van der Stelt, et al. 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. 2011 Oct 27;54(20):7350-62. [2]. Partha Mukhopadhyay, et al. The Novel, Orally Available and Peripherally Restricted Selective Cannabinoid CB2 Receptor Agonist LEI-101 Prevents Cisplatin-Induced Nephrotoxicity. Br J Pharmacol. 2016 Feb;173(3):446-58. |