JNJ-42226314

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。

JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain.

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.

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. Animal Model:Male C57Bl/6 mice weighing 20-30g and male Sprague-Dawley rats weighing 300-400 g Dosage:3 mg/kg and 30 mg/kg Administration:i.p.; 120 min Result:Dose-dependently elevated hippocampal 2-AG in vivo.

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Metabolic Enzyme/Protease

Lipase

Lipase

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1252765-13-1

489.56

C26H24FN5O2S

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (510.66 mM; 超声助溶 )

Fc1ccc(cc1)-n1ccc2cc(ccc12)C(=O)N1CC(C1)N1CCN(CC1)C(=O)c1nccs1

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(-20℃)

With Ice Pack

≥ 2 years