LEI-106
Dual DAGLα and ABHD6 inhibitor, a laboratory reagent.
Harm-reduction warning
No characterised human dose: animal / in vitro data only. Effect profile, safety margin and acute toxicity are not documented in human clinical practice. Extremely potent compound: severe effects, seizures and deaths reported in the literature.
C₂₆H₂₇NO₆S
CAS 1620582-23-1
- Family
- ECS pharmacological toolEnzyme inhibitor
- Molar mass
- 481.60 g/mol
Updated on
In plain terms
LEI-106 is a laboratory molecule, made by chemical synthesis: it exists neither in hemp nor in the human body. It is used to block the enzyme that makes 2-AG, one of the cannabinoids the brain produces itself, to observe what happens when this production falls. It is not a consumer product but a reagent reserved for research.
Receptors and activity
Target network
- Blocks or inhibits
The lower the cited value, the closer the target sits to LEI-106: one ring per factor of 100. A target with no measured value stays on the edge.
Cited values
- DAGLαInhibitorIC50 = 18 nM · human62 out of 100
Janssen et al., J Med Chem 2014 (ChEMBL values from document CHEMBL3352769) (new tab) · human DAGLα expressed in HEK293T cell membranes, surrogate substrate; Ki of 700 nM against the labelled natural substrate; IC50 of 124 nM on mouse brain DAGLα (ABPP)
- DAGLα (substrat naturel)Inhibitorno measured value cited
- ABHD6InhibitorKi = 800 nM · human35 out of 100
Janssen et al., J Med Chem 2014 (ChEMBL values from document CHEMBL3352769) (new tab) · human ABHD6 expressed in HEK293T cell membranes, 2-arachidonoylglycerol substrate
Pharmacology
LEI-106 belongs to the glycine sulfonamide family, a class of inhibitors of sn-1-diacylglycerol lipase α (DAGLα) found by high-throughput screening and then studied in Leiden (Janssen et al. 2014). DAGLα is the main enzyme producing 2-arachidonoylglycerol in the central nervous system. Its IC50 is 18 nM on human DAGLα with a surrogate substrate, but its inhibition constant is 700 nM against the natural substrate; ABHD6 is inhibited with a constant of 800 nM, and activity-based profiling showed at least three off-targets. Janssen et al. describe it as a potent dual inhibitor of DAGLα and ABHD6, and as a research lead for diet-induced obesity and metabolic syndrome, with no therapeutic result established. DAGLα inhibition is reversible (van der Wel et al. 2015). In female Sprague-Dawley rats, an intraperitoneal injection of 40 mg/kg lowered cortical 2-AG, reduced detection of the tight junction protein ZO-1, increased blood-brain barrier permeability to a sucrose tracer in cortical areas and increased constriction of the parenchymal microcirculation (Liktor-Busa et al. 2025). All these data are preclinical.
Key sources.
- Janssen FJ, Deng H, Baggelaar MP et al., Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6, J Med Chem 2014;57(15):6610-6622 (new tab)PMID 24988361
- van der Wel T, Janssen FJ, Baggelaar MP et al., A natural substrate-based fluorescence assay for inhibitor screening on diacylglycerol lipase α, J Lipid Res 2015 (new tab)PMID 25684760
- Liktor-Busa E, Levine AA, Young SJ et al., Inhibition of diacylglycerol lipase α induced blood-brain barrier breach in female Sprague-Dawley rats, J Physiol 2025;603(4):929-947 (new tab)PMID 39827410
- ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
- PubChem CID 102340761, LEI-106 (new tab)
History
- Source
- A synthetic molecule of the glycine sulfonamide class, absent from hemp and from any living organism. A research reagent for the endocannabinoid system.
Origin
Research tool
No biosynthetic pathway: the molecule does not come from any living organism; it is a synthetic glycine sulfonamide.
Legal framework
- European Union
A laboratory reagent; no European Union classification specific to the molecule was found in the sources consulted. Its status depends on the national law of each Member State.
- France
Not classified: absent from the ANSM list of narcotics (consolidated version updated 16/02/2026). A glycine sulfonamide without an indole, indazole or benzo[c]chromene nucleus, it falls under none of the generic entries of Annex IV. The absence of classification is not a marketing authorisation.
Sources: EUR-Lex, UNODC, CND, ANSM, IUPHAR/BPS, ChEBI, EUDA. Our method.
Classification
Family, origin and source verification
- Family
ECS pharmacological tool › Enzyme inhibitor
- Verification
Classification, sources and binding values checked on 20 October 2026; text read against its sources and Wikipedia.
- Wikipedia (English)
No dedicated article.
References
- Janssen FJ, Deng H, Baggelaar MP et al., Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6, J Med Chem 2014;57(15):6610-6622 (new tab)PMID 24988361
- van der Wel T, Janssen FJ, Baggelaar MP et al., A natural substrate-based fluorescence assay for inhibitor screening on diacylglycerol lipase α, J Lipid Res 2015 (new tab)PMID 25684760
- Liktor-Busa E, Levine AA, Young SJ et al., Inhibition of diacylglycerol lipase α induced blood-brain barrier breach in female Sprague-Dawley rats, J Physiol 2025;603(4):929-947 (new tab)PMID 39827410
- ANSM, Consolidated list of substances classified as narcotics, updated 16 February 2026, annex IV (new tab)
- PubChem CID 102340761, LEI-106 (new tab)
Identifiers
Names
- IUPAC name
- 2-[(2,2-dimethyl-3,4-dihydrochromen-6-yl)sulfonyl-[(4-phenoxyphenyl)methyl]amino]acetic acid
- Other names
- LEI 106 · N-((2,2-Dimethylchroman-6-yl)sulfonyl)-N-(4-phenoxybenzyl)glycine · CHEMBL3319620
Identifiers
- Formula
- C₂₆H₂₇NO₆S
- CAS
- 1620582-23-1
- PubChem CID
- 102340761(new tab)
- InChIKey
- FOEGBOXMDBPYEV-UHFFFAOYSA-N
- SMILES
- CC1(CCC2=
C(O1) C= CC(= C2) S(= O) (= O) N(CC3= CC= C(C= C3) OC4= CC= CC= C4) CC(= O) O) C
LLM ingestion format: a structured superset of the entry (identifiers, binding, versioned legal status). Full corpus.