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CAS No. : 2324160-91-8
MCE 国际站:MAGL-IN-1
产品活性:MAGL-IN-1 是一种有效,选择性,可逆和竞争性的 MAGL 抑制剂,IC50 值为 80 nM。MAGL-IN-1 对人乳腺癌,结肠直肠癌和卵巢癌细胞具有抗增殖作用。MAGL-IN-1 在体内和体外均可阻断 MAGL。
研究领域:Metabolic Enzyme/Protease
作用靶点:MAGL
In Vitro: MAGL-IN-1 (compound 23) (0.02-200 μM; 96 h) produces an appreciable inhibition of cell viability in all the tested cancer cell lines, with IC50s ranging from 7.9 to 57 μM.
MAGL-IN-1 (0.125-1 μM; 30 min) competitively binds to MAGL with 4-nitrophenylacetate, with a Ki of 39 nM.
MAGL-IN-1 (10 μM; 90 min) does not significantly inhibit CB1, CB2, FAAH, ABHD6 and ABHD12 activity at the concentration of 10 μM.
MAGL-IN-1 (1 nM-100 μM; 15 min) inhibits [3H]2-oleoyl glycerol (2-OG) hydrolysis in a concentration dependent manner in U937 cells, with an IC50 of 193 nM.
MAGL-IN-1 (0.01-30 μM; 15 min) inhibits 2-OG hydrolysis in a concentration-dependent manner in mouse brain membrane preparations, with an IC50 of 2.1 μM.
In Vivo: MAGL (compound 23) (50 mg/kg; a single i.p.) increases the 2-AG level in plasma and brain, and does not alter anandamide (AEA), arachidonic acid and prostaglandin levels in plasma and brain of mice.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Compound Library | Anti-Cancer Metabolism Compound Library | Lipid Metabolism Compound Library | Targeted Diversity Library | Anti-Colorectal Cancer Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | MAGL-IN-4 | PF-06795071 | KT185 | JZP-MA-11 | KT109 | JZL195 | DH-376 | JZP-430 | JW 642 | MJN110 | WWL123 analogue-1 | Euphol | MAGLi 432 | AA38-3 | KT203 | DO-264 | FAAH-IN-5 | SAR629 | LEI-106 | MAGL-IN-6 | Monoacylglycerol lipase inhibitor 1 | 7-Hydroxycoumarinyl arachidonate | FAAH/MAGL-IN-2 | ML-226 | ML-211 | Arachidonoyl Serinol | KML29 | FAAH/MAGL-IN-3 | MAGL-IN-5
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