LEI-106
Based on 1 Customer Validation
LEI-106 is a dual ABHD6 and DAGL-α inhibitor, with a Ki of 0.8 μM for ABHD6, and an IC50 of 18 nM and a Ki of 0.7 μM for DAGL-α. LEI-106 blocks the synthesis of 2-arachidonoylglycerol, reduces the level of endothelial cell-derived 2-arachidonoylglycerol, without altering the levels of cannabinoids and diacylglycerol. LEI-106 is applicable to research related to diet-induced obesity and metabolic syndrome.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.86%
- CAS 番号: 1620582-23-1
- 分子式: C26H27NO6S
- 分子量:481.56
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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DAGLα 18 nM (IC50) |
DAGLα 0.7 μM (Ki) |
ABHD6 0.8 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
18 nM
Compound: 15, LEI-106
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Inhibition of human DAGLalpha expressed in HEK293T cell membranes
Inhibition of human DAGLalpha expressed in HEK293T cell membranes
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[PMID: 24988361] |
LEI-106 (compound 15) potently inhibits human DAGL-α activity in cell-free HEK293 membranes, with an IC50 of 18 nM in a colorimetric assay and a Ki of 0.7 μM against the natural substrate[1].
LEI-106 (20 μM; 20 min) potently inhibits endogenous DAGL-α activity in mouse brain membrane homogenates, with an IC50 of 124 nM, and also acts as an inhibitor of ABHD6 in this system[1].
LEI-106 (30 min) potently inhibits human ABHD6 activity in cell-free HEK293T membranes, with a Ki of 0.8 μM against the natural substrate 2-AG[1].
LEI-106 (1.3 mM; 15 min) significantly reduces 2-AG levels in bEnd.3 mouse brain endothelial cells without altering AEA levels[2].
LEI-106 (650 μM-1.3 mM; 15 min) significantly increases PKC activity in bEnd.3 mouse brain endothelial cells[2].
LEI-106 (650 μM-1.3 mM; 15 min) induces VE-cadherin fragmentation in bEnd.3 mouse brain endothelial cells, with the 1.3 mM concentration also reducing full-length VE-cadherin, claudin-5, and ZO-1 levels; VE-cadherin fragmentation is mitigated by Rho-kinase inhibition but not calpain or PKC inhibition[2].
LEI-106 (650-1.3 mM; 2 min) significantly increases intracellular calcium levels in bEnd.3 mouse brain endothelial cells[2].
LEI-106 (650 μM; 15 min) significantly alters the phospho-proteome of bEnd.3 mouse brain endothelial cells, with changes in pathways related to mRNA processing, cytoskeletal organization, and Rho GTPase signaling[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:bEnd.3 mouse brain endothelial cells
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Concentration:650 μM; 1.3 mM
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Incubation Time:15 min
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Result:Caused no significant change in DAG levels compared to vehicle control at either concentration.
Significantly increased PKC activity at both concentrations compared to vehicle.
化学情報
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CAS 番号 1620582-23-1
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性状 Solid
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分子量 481.56
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分子式 C26H27NO6S
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Color White to off-white
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SMILES
OC(CN(CC1=CC=C(OC2=CC=CC=C2)C=C1)S(C3=CC=C4OC(C)(CCC4=C3)C)(=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (103.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Janssen FJ, 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. [Content Brief]
[2]. Levine AA, et al. Depletion of Endothelial-Derived 2-AG Reduces Blood-Endothelial Barrier Integrity via Alteration of VE-Cadherin and the Phospho-Proteome. Int J Mol Sci. 2023;25(1):531. Published 2023 Dec 30. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0766 mL | 10.3829 mL | 20.7658 mL | 51.9146 mL |
| 5 mM | 0.4153 mL | 2.0766 mL | 4.1532 mL | 10.3829 mL | |
| 10 mM | 0.2077 mL | 1.0383 mL | 2.0766 mL | 5.1915 mL | |
| 15 mM | 0.1384 mL | 0.6922 mL | 1.3844 mL | 3.4610 mL | |
| 20 mM | 0.1038 mL | 0.5191 mL | 1.0383 mL | 2.5957 mL | |
| 25 mM | 0.0831 mL | 0.4153 mL | 0.8306 mL | 2.0766 mL | |
| 30 mM | 0.0692 mL | 0.3461 mL | 0.6922 mL | 1.7305 mL | |
| 40 mM | 0.0519 mL | 0.2596 mL | 0.5191 mL | 1.2979 mL | |
| 50 mM | 0.0415 mL | 0.2077 mL | 0.4153 mL | 1.0383 mL | |
| 60 mM | 0.0346 mL | 0.1730 mL | 0.3461 mL | 0.8652 mL | |
| 80 mM | 0.0260 mL | 0.1298 mL | 0.2596 mL | 0.6489 mL | |
| 100 mM | 0.0208 mL | 0.1038 mL | 0.2077 mL | 0.5191 mL |
LEI-106 関連分類
HY-124314 関連分類
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