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JF-NP-26  

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包装规格：1g in glass bottle
产品描述：基本信息 产品编号： J10080  产品名称： JF-NP-26 CAS: 2341841-03-8   储存条件 粉末 -20℃ 四年 分子式： C30H28FN3O4 溶于液体 -80℃ 二年 分子量： 513.56     化学名：    Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   生物活性 产品描述 Raseglurant 的无活性光笼衍生物，也是第一个光笼 mGlu5 受体负性变构调节剂。在可见光波段 (405nm) 用光脉冲激发 JF-NP-26。JF-NP-26 诱导自由行为动物炎症性和神经病理性疼痛模型的光依赖性镇痛作用。 靶点 mGlu5 Receptor   体外研究 The authors assessed the JF-NP-26-mediated negative allosteric modulation of mGlu5 receptor-induced responses to the orthosteric agonist quisqualate,by using an inositol phosphate (IP) accumulation assay. while JF-NP-26 didn’t show activity in dark conditions,its negative allosteric modulator (NAM) activity is rescued upon 405nm visible light illumination (pIC50=7.1).Agonist challenge induced a robust mGlu5 receptor-mediated intracellular calcium rise both in dark and under 405nm illumination,which was blocked by raseglurant.JF-NP-26 is unable to restrain agonist-mediated signalling in dark conditions,it abolished mGlu5 receptor-mediated intracellular calcium accumulation upon 405nm irradiation,thus demonstrating a light-dependent negative allosteric modulator activity. 体内研究 JF-NP-26 (10mg/kg;i.p.;irradiated at 405nm (or dark) for 5 min) significantly increased pain thresholds in CCI mice only after thalamic irradiation.JF-NP-26 (10mg/kg;i.p.;at 405nm light (or dark) for 5 min) shows light-dependent analgesic efficacy in neuropathic pain.Systemic administration and in vivo photoactivation of JF-NP-26 does not impair memory in mouse. Animal Model: Adult male C57BL/6J mice weighing 20-25g (chronic constriction injury (CCI) model) Dosage: 10mg/kg Administration: I.p.;irradiated at 405nm (or dark) for 5 min Result: Significantly increased pain thresholds in CCI mice only after thalamic irradiation.   Animal Model: Formalin animal model of pain adult male CD-1 mice Dosage: 10mg/kg Administration: I.p.;at 405nm light (or dark) for 5 min Result: Unable to promote antinociception in dark conditions,it elicited antinociception following direct hind paw irradiation both at phase I (5 min after formalin injection in the hind paw) and phase II (20–30 min after formalin injection).
保存条件：-20℃

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