103878-84-8

Basic information

• Product Name: LAZABEMIDE
• Synonyms: LAZABEMIDE;LAZABEMIDE HYDROCHLORIDE;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide;Ro-19-6327;2-PyridinecarboxaMide, N-(2-aMinoethyl)-5-chloro-;Ro 19-6327/000;Lazabemide hydrate;N-(2-Aminoethyl)-5-chloro-2-pyridinecarboxamide hydrate
• CAS NO: 103878-84-8
• Molecular Formula: C8H10ClN3O
• Molecular Weight: 199.64
• Mol File: 103878-84-8.mol
• Article Data: 4

Chemical Properties

• Boiling Point: 397.4 °C at 760 mmHg
• Flash Point: 194.2 °C
• Appearance: white to tan/
• Density: 1.286 g/cm³
• Vapor Pressure: 1.59E-06mmHg at 25°C
• Refractive Index: 1.571
• Storage Temp.: room temp
• Solubility: DMSO: ≥22mg/mL
• PKA: 12.90±0.46(Predicted)
• CAS DataBase Reference: LAZABEMIDE(CAS DataBase Reference)
• NIST Chemistry Reference: LAZABEMIDE(103878-84-8)
• EPA Substance Registry System: LAZABEMIDE(103878-84-8)

Safety Data

• Hazard Codes: Xn
• Statements: 22-36
• Safety Statements: 26
• WGK Germany: 3
• Hazardous Substances Data: 103878-84-8(Hazardous Substances Data)

Usage

Uses

Lazabemide hydrate may be used in cell signaling studies.

Biochem/physiol Actions

Lazabemide is effective in treatment of Alzheimer′s disease and in combination with nicotine replacement therapy aids in smoking cessation.

InChI:InChI=1/C8H10ClN3O/c9-6-1-2-7(12-5-6)8(13)11-4-3-10/h1-2,5H,3-4,10H2,(H,11,13)

Upstream product

• 86873-60-1 5-chloropicolinic acid 
• 128073-03-0 4-chloronicotinoyl chloride 
• 107-15-3 ethylenediamine 
• 943621-63-4 2-(5-chloropyridine-2-yl)-1H-imidazoline 

Related news

Design, synthesis and biological evaluation of LAZABEMIDE (cas 103878-84-8) derivatives as inhibitors of monoamine oxidase07/21/2019

In the studied a series novel of lazabemide derivatives were designed, synthesized and evaluated as inhibitors of monoamine oxidase (MAO-A or MAO-B). These compounds used lazabemide as the lead compound, and the chemistry structures were modified by used the bioisostere and modification of compo...detailed

Relevant articles and documents

Design, synthesis and biological evaluation of lazabemide derivatives as inhibitors of monoamine oxidase

In the studied a series novel of lazabemide derivatives were designed, synthesized and evaluated as inhibitors of monoamine oxidase (MAO-A or MAO-B). These compounds used lazabemide as the lead compound, and the chemistry structures were modified by used the bioisostere and modification of compound with alkyl principle. The two types of inhibitors (inhibition of MAO-A and inhibition of MAO-B) were screened by inhibition activity of MAO. In vitro experiments showed that compounds 3a, 3d and 3f had intensity inhibition the biological activity of MAO-A, while compounds 3i and 3m had intensity inhibition the biological activity of MAO-B. It could be seen from the data of inhibition activity experiments in vitro, that the compound 3d was IC50 = 3.12 ± 0.05 μmol/mL of MAO-A and compound 3m was IC50 = 5.04 ± 0.06 μmol/mL. In vivo inhibition activity experiments were conducted to evaluate the inhibitory activity of compounds 3a, 3d, 3f, 3i and 3m by detecting the contents of 5-HT, NE, DA and activity of MAO-A and MAO-B in plasma and brain tissue. In vivo inhibition activity evaluation results showed that the compounds 3a, 3d, 3f, 3i and 3m had increased the contents of 5-HT, NE and DA in plasma and brain tissues. Meanwhile, the determination results activity of MAO in plasma and brain tissue showed that the compounds 3a, 3d, and 3f had a significant inhibitory effect on the activity of MAO-A, while the compounds 3i and 3m showed inhibitory effect on the activity of MAO-B. This study provided a new inhibitors for inhibiting of MAO activity.

PHARMACEUTICAL PREPARATIONS OF CRYSTALLINE LAZABEMIDE

Pharmaceutical compositions of lazabemide HCl crystalline Form A are disclosed along with methods of their production.