货号:A216404
同义名:
ABR-215062; LAQ
Laquinimod is an orally administered neuroimmunomodulator initially developed for the treatment of multiple sclerosis.
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描述 | Laquinimod is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. In vivo laquinimod treatment inhibited donor myelin-specific T cells from transferring EAE (experimental autoimmune encephalomyelitis) to naive recipient mice. In vivo laquinimod treatment altered subpopulations of myeloid antigen presenting cells (APC) that included a decrease in CD11c(+)CD11b(+)CD4(+) dendritic cells (DC) and an elevation of CD11b(hi)Gr1(hi) monocytes[3]. Topical administration of laquinimod to the injured corneas dramatically inhibited alkali-induced corneal neovascularization and decreased inflammatory cell (such as macrophage) infiltration in a corneal injury mouse model. Laquinimod significantly downregulated the expression of chemokines (monocyte chemotactic protein-1 and macrophage inflammatory protein-1), pro-inflammatory cytokines (interleukin-1β and tumor necrosis factor-alpha), vascular endothelial growth factor, nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing 3 and apoptosis-associated speck-like protein containing C-terminal caspase-recruitment domain adaptor protein in both injured corneas and RAW cells. In vitro, laquinimod also dramatically inhibited the proliferation, migration and tube formation of human umbilical vein endothelial cells[4]. Laquinimod had a significant protective impact against MPP+-induced neurotoxicity. Laquinimod prevented MPP+-induced reduction of cell proliferation, the release of lactate dehydrogenase (LDH), and apoptosis[5]. Laquinimod protects against glutamate excitotoxicity of the cerebellum of EAE mice by bursting the expression of glial glutamate transporters, independently of its anti-inflammatory effects[6]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01404117 | Relapsing Multiple Sclerosis | Phase 2 | Withdrawn(Study is being redes... 展开 >>igned) 收起 << | January 2014 | - |
NCT00605215 | Multiple Sclerosis | Phase 3 | Completed | - | - |
NCT01707992 | Multiple Sclerosis | Phase 3 | Completed | - | - |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.80mL 0.56mL 0.28mL |
14.01mL 2.80mL 1.40mL |
28.03mL 5.61mL 2.80mL |
CAS号 | 248281-84-7 |
分子式 | C19H17ClN2O3 |
分子量 | 356.8 |
SMILES Code | C1=CC=C(Cl)C2=C1N(C(=C(C2=O)C(=O)N(CC)C3=CC=CC=C3)O)C |
MDL No. | MFCD08689859 |
别名 | ABR-215062; LAQ; TV-5600; SAIK-MS |
运输 | 蓝冰 |
InChI Key | GKWPCEFFIHSJOE-UHFFFAOYSA-N |
Pubchem ID | 54677946 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry, room temperature |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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