LEI 101 hydrochloride

Name: LEI 101 hydrochloride
Brand: Tocris Bioscience
SKU: 5826

Tocris Bioscience, part of Bio-Techne | Catalog # 5826

COA / SDS

Potent and selective CB2 partial agonist; orally biovailable

Key Product Details

Description:	Potent and selective CB₂ partial agonist; orally biovailable
Chemical Name:	3-Cyclopropyl-1-[[4-[6-[(1,1-dioxido-4-thiomorpholinyl)methyl]-5-fluoro-2-pyridinyl]phenyl]methyl]-2,4-imidazolidinedione hydrochloride
Purity:	≥98% (HPLC)
Molecular Weight:	508.99

View Full Technical Details for LEI 101 hydrochloride

Technical Data
Citations

Biological Activity for LEI 101 hydrochloride

LEI 101 hydrochloride is a 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.

Technical Data for LEI 101 hydrochloride

M. Wt	508.99
Formula	C₂₃H₂₅FN₄O₄S.HCl
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2250025-91-1
PubChem ID	127021038
InChi Key	APLLNJWPLUIBCG-UHFFFAOYSA-N
Smiles	FC1=CC=C(C2=CC=C(C=C2)CN3CC(N(C3=O)C4CC4)=O)N=C1CN5CCS(=O)(CC5)=O.Cl

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.

Solubility for LEI 101 hydrochloride

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	50.9	100

Preparing Stock Solutions for LEI 101 hydrochloride

The following data is based on the product molecular weight 508.99.

Batch specific molecular weights may vary from batch to batch due to the degree 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	0.20 mL	0.98 mL	1.96 mL
50 mM	0.04 mL	0.20 mL	0.39 mL

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References for LEI 101 hydrochloride

References are publications that support the biological activity of the product.

Mukhopadhyay The novel, orally available and peripherally restricted selective cannabinoid CB₂ receptor agonist LEI-101 prevents cisplatin-induced nephrotoxicity. Br.J.Pharmacol. 2016 PMID: 26398481
van der Stelt M 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 PMID: 21923175