生化/生理作用
Brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL).
JNJ-42226314 is a brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL)(IC50 = 1.1) that exhibits antinociceptive efficacy in the rat models neuropathic and inflammatory pain. JNJ-42226314 elevates hippocampal 2-arachidonoylglycerol (2-AG) levels and prolongs wakefulness in rats.
JNJ-42226314 is a brain penetrant, highly selective and potent reversible inhibitor of monoacylglycerol lipase (MAGL)(IC50 = 1.1) that exhibits antinociceptive efficacy in the rat models neuropathic and inflammatory pain. JNJ-42226314 elevates hippocampal 2-arachidonoylglycerol (2-AG) levels and prolongs wakefulness in rats.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
The discovery of azetidine-piperazine di-amides as potent, selective and reversible monoacylglycerol lipase (MAGL) inhibitors
Bioorganic & Medicinal Chemistry Letters, 30(14), 127243-127243 (2020)
The Journal of pharmacology and experimental therapeutics, 372(3), 339-353 (2019-12-11)
The serine hydrolase monoacylglycerol lipase (MAGL) is the rate-limiting enzyme responsible for the degradation of the endocannabinoid 2-arachidonoylglycerol (2-AG) into arachidonic acid and glycerol. Inhibition of 2-AG degradation leads to elevation of 2-AG, the most abundant endogenous agonist of the
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