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MAGL-IN-1

CAS No. : 2324160-91-8

MCE 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 K_i 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.

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