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CAS No. : 2135785-20-3
MCE 国际站:MAGL-IN-4
产品活性:MAGL-IN-4 是一种口服有效,选择性和可逆的单酰基甘油脂肪酶 (MAGL) 抑制剂,IC50 为 6.2 nM。MAGL-IN-4 可以穿透血脑屏障 (BBB)。MAGL-IN-4 主要通过大脑中选择性抑制 MAGL 增加 2-花生四烯酰甘油 (2-AG) 水平来增强内源性大麻素信号。
研究领域:Metabolic Enzyme/Protease
作用靶点:MAGL
In Vitro: MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL.
MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA).
In Vivo: MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | CNS-Penetrant Compound Library | Orally Active Compound Library | Anti-Cancer Metabolism Compound Library | Lipid Metabolism Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | 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 | MAGL-IN-1 | FAAH/MAGL-IN-3 | MAGL-IN-5
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