LEI 101 hydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 5826 - LEI 101 hydrochloride | C23H25FN4O4S.HCl
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)
Datasheet
Citations
Reviews
Literature

Biological Activity

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

M. Wt 508.99
Formula C23H25FN4O4S.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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

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Product Datasheets

Safety Datasheet

References

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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Literature in this Area

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