LEI 101 hydrochloride

Pricing Availability   Qty
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)
Literature (1)

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
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 Data for LEI 101 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
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.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets for LEI 101 hydrochloride

References for LEI 101 hydrochloride

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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Citations for LEI 101 hydrochloride

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Literature in this Area

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Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.