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CAS No. : 1252765-13-1
MCE 国际站:JNJ-42226314
产品活性:JNJ-42226314 是一种竞争性,高度选择性和可逆的非共价单酰甘油脂肪酶 MAGL 抑制剂。JNJ-42226314 可剂量依赖性增强主要的内源性大麻素 2-花生四烯酰甘油 (2-AG),在神经性和炎性疼痛模型中表现出抗伤害作用。
研究领域:Metabolic Enzyme/Protease
作用靶点:MAGL
In Vitro: JNJ-42226314 has IC50s of 1.13 nM, 1.88 nM, 0.67 nM, 0.97 nM for human Hela cells, human PBMC, mouse brain and rat brain, respectively.
In Vivo: JNJ-42226314 (i.p.; 3 mg/kg and 30 mg/kg; 120 min) dose-dependently elevates hippocampal 2-AG in vivo.
JNJ-42226314 (i.p.; 30 mg/kg)significantly increases total wake time for up to 8 hours afterward, whereas total wake time was only elevated for 2 hr following a 3 mg/kg dose.
JNJ-42226314 (i.p.; 30 mg/kg) is antinociceptive in the rat complete Freund’s adjuvant (CFA) model of inflammatory pain.
JNJ-42226314 has t1/2 values of 11.4, 27.6, 27.2 min for MAGL in human, mouse and rat, respectively.
相关产品:Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Anti-Cancer Metabolism Compound Library | Lipid Metabolism 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 | MAGL-IN-1 | FAAH/MAGL-IN-3 | MAGL-IN-5
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