LEI-101 

LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC₅₀ of 8 for hCB2, and a pK_i of less than 4 for hERG. LEI-101 is ~100-fold more potent in binding to CB2 receptors than to CB1 receptors^[1][2].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

508.99

C₂₃H₂₆ClFN₄O₄S

2250025-91-1

O=C1N(C2CC2)C(CN1CC3=CC=C(C4=NC(CN5CCS(CC5)(=O)=O)=C(F)C=C4)C=C3)=O.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]