常用名 | JZL 184 | CAS号 | 1101854-58-3 |
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价格 | ¥需询单/1kg | 纯度 | 97.0% |
备货期 | 需询单 | 库存 | 询单 |
产品网页 | http://www.kylpharm.com/index.php?s=/Home/Article/detail/id/762.html |
产品详情(用途,包装等)
用途: JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.IC50 value: 8 nM [1]Target: MAGL inhibitorin vitro: JZL184 prolongs DSE in Purkinje neurons in cerebellar slices and DSI in CA1 pyramidal neurons in hippocampal slices. JZL184 is more potent in inhibiting mouse MAGL than rat MAGL [2]. in vivo: When administered to mice at 16 mg/kg, intraperitoneally, JZL 184 reduces MAGL activity by 85%, elevates brain 2-AG levels by 8-fold, and elicits analgesic activity in a variety of pain assays that qualitatively mimics direct central cannabinoid (CB1) agonists [1]. Acute administration of JZL184 to FAAH(-/-) mice enhanced the magnitude of a subset of cannabimimetic responses, repeated JZL184 treatment led to tolerance to its antinociceptive effects, cross-tolerance to the pharmacological effects of Δ(9)-tetrahydrocannabinol, decreases in CB1 receptor agonist-stimulated guanosine 5'-O-(3-[(35)S]thio)triphosphate binding, and dependence as indicated by rimonabant-precipitated withdrawal behaviors, regardless of genotype [3]. 物理化学性质: CAS号:1101854-58-3 常用中文名:JZL 184 常用英文名:JZL184 分子式:C27H24N2O9 分子量:520.487 密度:1.5±0.1 g/cm3 沸点:706.4±60.0 °C at 760 mmHg 熔点:N/A 闪点:381.0±32.9 °C 储存条件:-20℃ |