A potent inhibitor of sn-1 DAGLα
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LEI-106

Item No. 16419

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-6-yl)sulfonyl]-N-[(4-phenoxyphenyl)methyl]-glycine
CAS Number
1620582-23-1
Molecular Formula
C26H27NO6S
Formula Weight
481.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 50 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 30 mg/mlEthanol: 0.1 mg/ml
λmax
245 nm
SMILES
OC(CN(S(C1=CC=C(OC(C)(C)CC2)C2=C1)(=O)=O)CC(C=C3)=CC=C3OC4=CC=CC=C4)=O
InChi Code
InChI=1S/C26H27NO6S/c1-26(2)15-14-20-16-23(12-13-24(20)33-26)34(30,31)27(18-25(28)29)17-19-8-10-22(11-9-19)32-21-6-4-3-5-7-21/h3-13,16H,14-15,17-18H2,1-2H3,(H,28,29)
InChi Key
FOEGBOXMDBPYEV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol (2-AG; Item No. 62160) by attacking DAG at the sn-1 position. LEI-106 is a potent in vitro inhibitor of sn-1 DAGLα (IC50 = 18 nM).1 It blocks the hydrolysis of sn-1-oleoyl-2-AG, the natural substrate of DAGLα, with a Ki value of 0.7 µM.1 LEI-106 inhibits the hydrolysis of 2-AG by the monoacylglycerol lipase ABHD6 in mouse brain membrane homogenates and in HEK293T cell membrane preparations (Ki = 0.8 µM).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Janssen, F.J., Deng, H., Allarà, M., et al. Discovery of glycine sulfonamides as dual inhibitors of sn-1-diacylglycerol lipase α and α/β-hydrolase domain 6. J. Med. Chem. 57(15), 6610-6622 (2014).