103878-83-7
基本信息
Ro 19-6327/001
JMFKTFLARGGXCC-UHFFFAOYSA-N
N-(2-Aminoethyl)-5-chlor-2-pyridincarbox
N-(2-Aminoethyl)-5-chlor-2-pyridincarboxamid-hydrochlorid
N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrochloride
2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-, Monohydrochloride
物理化学性质
| 熔点 | 193-195° |
| 储存条件 | Desiccate at RT |
| 溶解度 | Soluble to 100 mM in water and to 100 mM in DMSO |
| 酸度系数(pKa) | 8.9(at 25℃) |
| 形态 | 粉末 |
安全数据
| 毒性 | LD50 orally in mice: 1000-2000 mg/kg (Imhof, Kyburz, 1986) |
拉扎贝胺盐酸盐价格(试剂级)
| 报价日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
| 2024/11/08 | S6422 | 拉扎贝胺盐酸盐 Lazabemide | 103878-83-7 | 25mg | 1286.7元 |
常见问题列表
| Target | Value |
|
MAO-B
(Cell-free assay) | 7.9 nM(Ki) |
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.