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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Monoacylglycerol Lipase (MAGL)-JNJ-42226314
JNJ-42226314

Chemical Structure : JNJ-42226314

CAS No.: 1252765-13-1

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JNJ-42226314 (JNJ42226314)

货号: PC-72112Not For Human Use, Lab Use Only.

JNJ-42226314 (JNJ42226314) is a potent, highly selective and reversible MAGL inhibitor with IC50 of 1.13 nM (hMAGL).

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1680 In stock
25 mg ￥2580 In stock
50 mg ￥3980 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-42226314 (JNJ42226314) is a potent, highly selective and reversible MAGL inhibitor with IC50 of 1.13 nM (hMAGL).
JNJ-42226314 displays high selectivity against the serine hydrolase superfamily, as well as a panel of 50 binding assays for ion channels and receptors, including CB1 and CB2. JNJ-42226314 also shows MAGL across species (mouse, rat MAGL IC50=1 nM).
JNJ-42226314 inhibits MAGL in a competitive mode with respect to the 2-AG substrate.
JNJ-42226314 time- and dose-dependently bound to MAGL, indirectly led to CB1 occupancy by raising 2-AG levels, and raised norepinephrine levels in cortex in rodent brain.
JNJ-42226314 exhibited antinociceptive efficacy in both the rat complete Freund's adjuvant-induced radiant heat hypersensitivity and chronic constriction injury-induced cold hypersensitivity models of inflammatory and neuropathic pain, respectively.
JNJ-42226314 induced hippocampal synaptic depression, altered sleep onset, and decreased electroencephalogram gamma power at 30 mg/kg, significantly increased 2-AG and norepinephrine levels, and produced neuropathic antinociception without synaptic depression at 3 mg/kg.

物理化学性质&存储条件

分子量 489.569
分子式 C26H24FN5O2S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(1-(4-Fluorophenyl)-1H-indol-5-yl)(3-(4-(thiazole-2-carbonyl)piperazin-1-yl)azetidin-1-yl)methanone

参考文献

1. Ryan M Wyatt, et al. J Pharmacol Exp Ther. 2020 Mar;372(3):339-353.

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