103878-84-8
基本信息
N-(2-氨基乙基)-5-氯-2-吡啶羧酰胺
LAZABEMIDE
Ro 19-6327/000
Lazabemide hydrate
Ro 19-6327 hydrate
LAZABEMIDE HYDROCHLORIDE
N-(2-aminoethyl)-5-chloropyridine-2-carboxamide
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide
2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate
物理化学性质
| 外观性状 | 单盐酸拉扎贝胺(Lazabemide Monohydrochloride)：C8Hl0ClN3O?HCl。[103878-83-7]。从甲醇-乙醚结晶，熔点193～195℃。分配系数(正辛醇脉)：约0.1。pKa 8.9。急性毒性LD50小鼠(mg/kg)：1000~2000口服。 |
| 沸点 | 397.4±37.0 °C(Predicted) |
| 密度 | 1.286±0.06 g/cm3(Predicted) |
| 储存条件 | room temp |
| 溶解度 | 二甲基亚砜：≥22mg/mL |
| 酸度系数(pKa) | 12.90±0.46(Predicted) |
| 形态 | 粉末 |
| 颜色 | 白色至棕褐色 |
| InChI | 1S/C8H10ClN3O.H2O/c9-6-1-2-7(12-5-6)8(13)11-4-3-10;/h1-2,5H,3-4,10H2,(H,11,13);1H2 |
| InChIKey | JYWYNPKXSLPWGV-UHFFFAOYSA-N |
| SMILES | O.NCCNC(=O)c1ccc(Cl)cn1 |
安全数据
| 危险性符号(GHS) |  GHS07 |
| 警示词 | 警告 |
| 危险性描述 | H302-H319 |
| 防范说明 | P264-P270-P280-P301+P312-P305+P351+P338-P337+P313 |
| 危险品标志 | Xn |
| 危险类别码 | 22-36 |
| 安全说明 | 26 |
| WGK Germany | 3 |
| 存储类别 | 11 - Combustible Solids |
| 危险性类别 | Acute Tox. 4 Oral Eye Irrit. 2 |
应用领域
制备方法
拉扎贝胺价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2025/12/22 | HY-14201 | 拉扎贝胺 Lazabemide | 103878-84-8 | 5 mg | 312元 |
| 2025/12/22 | HY-14201 | 拉扎贝胺 Lazabemide | 103878-84-8 | 10mg | 500元 |
| 2025/12/22 | HY-14201 | 拉扎贝胺 Lazabemide | 103878-84-8 | 10mM * 1mLin DMSO | 550元 |
常见问题列表
IC50: 30 nM (MAO-B).
The in vitro binding characteristics of both radiolabeled inhibitors revealed them to be selective, high-affinity ligands for the respective enzymes. K D and B max values for 3 H-Ro 19-6327 in rat cerebral cortex are 18.4 nM and 3.45 pmol/mg protein, respectively. The IC 50 values for lazabemide are: 86 μM for NA uptake; 123 μM for 5HT uptake; > 500 μM for DA uptake, respectively.. Lazabemide (5 μM) inhibits human MAO-B and MAO-A with IC 50 of 6.9 nM and >10 nM, respectively. And it inhibits rat MAO-B and MAO-A with IC 50 of 37 nM and >10 μM, respectively ina enzymatic assay.Lazabemide differs from L-deprenyl in their ability to induce release of endogenous monoamines from synaptosomes. Thus, Lazabemide (500 μM) 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 (250 nM) results in a clear inhibition of DOPAC formation, while does not increase the accumulation of newly-formed DA in those tubular epithelial cells loaded with 50 microM L-DOPA.
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.