NF 1819

NF 1819 是一种有效且选择性的不可逆 MGL（&#946；-内酰胺基单酰基甘油脂肪酶）抑制剂。

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库存: 现货

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数量
10mg

￥2325.00

1860.00

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已选 0 种 0 瓶

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Background

Potent and selective irreversible MAGL inhibitor (IC50 values are 0.25 and 7.4 nM at rMAGL and hMAGL, respectively). Exhibits 389-fold selectivity over hFAAH and exhibits minimal binding at CB receptors (IC50 > 10 μM). Alleviates symptoms in a MS in vivo model. Exhibits analgesic effects in an acute inflammatory pain model in vivo. Ameliorates neuropathic hypersensitivity induced by oxaliplatin . Displays high membrane permeability and brain penetrant.

Brindisi et al (20106) Development and pharmacological characterization of selective blockers of 2-arachidonoyl glycerol degradation with efficacy in rodent models of multiple sclerosis and pain. J.Med.Chem. 59 2612 PMID:26888301