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Lazabemide hydrochloride  ≥98%

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包装规格：25mg 100mg 250mg in glass bottle
产品描述：基本信息 产品编号： L11031 产品名称： Lazabemide hydrochloride CAS: 103878-83-7   储存条件 粉末 -20℃ 四年     分子式： CH11Cl2N3O 溶于液体     分子量 236.10     化学名：  2-Pyridinecarboxamide, N-(2-aminoethyl)-5-chloro-, hydrochloride (1:1);2-Pyridinecarboxamide, N-(2-aminoethyl)-5-chloro-, hydrochloride (1:1) 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 一种单胺氧化酶 B (MAO-B) 的选择性的可逆抑制剂(IC50=0.03μM)，但对 MAO-A (IC50>100μM) 活性较低。高浓度 Lazabemide 具有抑制单胺摄取的作用，抑制去甲肾上腺素、血清素和多巴胺摄取的 IC50 值分别为 86μM、123μM 和 >500μM。Lazabemide 可用于帕金森和阿尔茨海默病的研究。 靶点 MAO-B 0.4nM (IC50) 体外研究 The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. KD and Bmax values for 3H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC50 values for lazabemide are: 86 μM for NA uptake; 123μM for 5HT uptake; > 500μM for DA uptake, respectively. Lazabemide (5μM) inhibits human MAO-B and MAO-A with IC50 of 6.9nM and >10nM, respectively. And it inhibits rat MAO-B and MAO-A with IC50of 37nM and >10μM, respectively ina enzymatic assay. Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500μM) induces a greater 5 HT release than does L-deprenyl, but is less effective than L-deprenyl in releasing DA. On the contrary, lazabemide was almost completely inactive on either 5 HT and DA release. Lazabemide (250nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newlyformed DA in those tubular epithelial cells loaded with 50microM L-DOPA. 体内研究 Lazabemide (3 mg/kg) attenuates ichemia reperfusion-induced hydroxyl radical generation and pretreatment with Lazabemide showed decreased DOPAC levels in comparison with those of their respective vehicle-treated control groups.
保存条件：-20℃

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